Archive for the ‘HT Screening’ Category
Cisbio has entered into a partnership agreement with Lumiphore to gain access to new fluorescence reporter molecules for use in its high throughput (HT) screening assays.
Last Updated on Tuesday, 11 September 2007 03:40 Written by Fred Tuesday, 11 September 2007 03:40
The agreement grants Cisbio exclusive access to the Lumi4 compounds for fluorescence applications in drug discovery, with Lumiphore free to develop partnerships to develop the technology in other areas.
Cisbio has played an important part in the development of HT drug screening technologies and has enabled researchers to conduct binding assays based on its homogenous time-resolved fluorescence (HTRF) system that combines Time-Resolved Fluorescence (TRF) and Fluorescence Resonance Energy Transfer (FRET).
“This agreement reinforces our position as real leaders the TR-FRET field, and is a very important step for us,” said François Degorce, head HTRF marketing and business development at Cisbio.
“We have plans to apply the technology in some of our current products as well as many of our mid-to-long term projects.”
Lumiphore’s lanthanide-based florescent reporter molecules will enable Cisbio to generate assays that provide more accurate results due to their long-emission lifetimes and strong luminescent properties that provide higher signal-to-noise (S/N) ratio.
“According the last figures I have, TR-FRET accounted for between 13 and 15 per cent of the HT screening market and the use of this technology is increasing rapidly compared with other competing technologies due to its increased sensitivity and robustness,” said Degorce.
During the TR-FRET process, fluorescent reporting molecules emit long-lived fluorescence signals when a fluorescence donor molecule binds to an acceptor / emitter molecule.
This is in contrast to many biological assay systems that use radioactive reagents, which pose health risks not just to the researchers themselves, but also to any live cell lines they may be conducting assays in.
The donor / acceptor molecules and proteins can be supplied from the company’s catalogue, or can be developed in-house or by Cisbio to enable researchers to study the binding of potential drug candidates.
This powerful new technology brings researchers increased assay sensitivity, higher throughput and greater reliability and flexibility than some other systems with Cisbio already providing a wide range of assays based on its original Europium cryptate technology.
These include assays for GPCRs (G Protein couple receptors), inflammation, metabolic diseases, central nervous system, biomarkers, kinase assays and other oncology related assays.
“The new technology will complement our existing catalogue offerings and quite a few of our existing assays will be upgraded to make use of it,” said Degorce.
In addition, the company also offer kits for monitoring bioprocesses such as protein or antibody engineering as well as enabling rapid quantification of antibodies during the production process.
“The Lumiphore technology is very bright and very stable, and will enable an upgraded version of the HTRF assays to be conducted on a expanded range of detection platforms,” said Degorce.
He continued by saying that because the Lumiphore technology uses a Terbium ion rather than the Europium ion that Cisbio currently uses a whole range of new possibilities could be accessed.
This could include the development of multicolour assays that use different donor-acceptor pairs that have very narrow excitation and emission bands.
The compounds resistance to bleaching allows samples to be archived allowing improved quality control comparisons between old and new data – a problem for more easily bleached organic dyes.
“When you run a screen with 100,000 samples and the detector system is not working properly, instead of throwing the plate away and having to start again because the lifetime of the dyes are too short lived to conduct the experiments the next day, you can store the plates in the fridge or freezer and study the plates the next week when the detector is back up and running,” said Degorce.
“Many luminescence screens actually destroy the reporter molecules such that any repeat read-outs are less sensitive than the first, with both our old Europium cryptate dye and this new Lumiphore technology you can just keep on reading the plates.”
Posted under Collaborations, Europe, HT Screening, North America, Press Releases | Comments Off
Cisbio international’s upcoming third annual “HTRF® In Drug Discovery†Symposium will be held September 26-28 in Sonoma, California
Last Updated on Thursday, 19 July 2007 02:13 Written by Fred Thursday, 19 July 2007 02:13
Over the course of three days, experts in drug screening from around the globe will assemble to discuss the latest applications of Cisbio’s proprietary HTRF® technology in the drug screening, target discovery and mechanistic fields. A number of scientific sessions will specifically examine GPCR and kinase screening, cell-based biomarker detection and functional assays.Â
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HTRF® (homogenous time-resolved fluorescence) technology is a highly sensitive, robust technology for the detection of molecular interactions and is widely used for the high throughput stage of drug development. As part of its ongoing commitment to providing the highest quality technical support to HTRF® customers, Cisbio established its annual symposium in 2005 as a forum for exchanging ideas on drug screening and the latest in HTRF® innovation
Posted under Compound Libraries, Europe, HT Screening, Targeted Libraries | Comments Off
DiscoveRx, a Leader in GPCR Assays, Launches a 30 Second Assay for Beta-Arrestin Based ScreeningWith the PathHunter(TM) Flash Detection Kit
Last Updated on Sunday, 29 April 2007 06:04 Written by admin Friday, 27 April 2007 06:38
DiscoveRx, a Leader in GPCR Assays, Launches a 30 Second Assay for Beta-Arrestin Based ScreeningWith the PathHunter(TM) Flash Detection Kit, beta-arrestin recruitment by a GPCR can now be detected in 30 seconds, permitting screens of up to 1,000,000 compounds in 48 hours. Unlike lengthy reporter gene assays, PathHunter beta-arrestin assays are direct and hence minimize the opportunity for off-target effects. A ligand-activated, GPCR-arrestin interaction combines two beta-galactosidase fragments, enabling rapid chemiluminescent detection in a homogeneous format. The kit is designed for whole class of plate readers with onboard fluidics and flash detection mode.
With the PathHunter(TM) Flash Detection Kit, beta-arrestin recruitment by a GPCR can now be detected in 30 seconds, permitting screens of up to 1,000,000 compounds in 48 hours. Unlike lengthy reporter gene assays, PathHunter beta-arrestin assays are direct and hence minimize the opportunity for off-target effects. A ligand-activated, GPCR-arrestin interaction combines two beta-galactosidase fragments, enabling rapid chemiluminescent detection in a homogeneous format. The kit is designed for whole class of plate readers with onboard fluidics and flash detection mode.
Additionally, screening campaigns can be accelerated by conducting beta-arrestin and calcium assays in the same well on same instrument, without need of cell fixation, when using instruments capable of real-time fluorescence and flash chemiluminescence. The ability to run intracellular calcium assays in combination with the homogeneous, chemiluminescent PathHunter beta-Arrestin assay helps drive the costs of primary screening campaigns down while significantly increasing the speed of compound characterization. Either run alone or in combination with calcium mobilization, with launch of the Flash Kit, GPCR Screening has now become even faster. With an expanding list of GPCR Beta-Arrestin assays (greater than 90 assays) being added to its product offering, DiscoveRx has a solution for virtually any GPCR screening campaign. Standard chemiluminescent detection for batch mode processing or flash detection for kinetic measurements, we have a solution for you! Call us to discuss your GPCR screening needs!
Founded in 2000, DiscoveRx is a privately held, venture-backed company headquartered in Fremont, California, with an additional office in Birmingham, England. The Company pioneered the use of beta-galactosidase enzyme fragment complementation in biochemical and cell based assays for discovery research, and holds extensive intellectual property in this area. DiscoveRx is dedicated to the development and commercialization of innovative solutions to study GPCRs, Kinases and other major drug target classes, and many of their innovative products have been widely adopted in pharmaceutical and biotech drug screening laboratories worldwide. The Company is also the recipient of Frost and Sullivan’s prestigious 2006 Award for Technology Innovation. This award was given in recognition for successful introduction of PathHunter(TM) cell-based assay platform and company’s overall work on intact and/or lysed cell based assays. For more information on DiscoveRx products, please visit www.discoverx.com
Posted under Europe, HT Screening, North America, Press Releases, Targeted Libraries | Comments Off
Shrinking screening for drugs
Last Updated on Wednesday, 11 April 2007 10:55 Written by admin Wednesday, 11 April 2007 10:55
Scientists in the US have found a way to screen for potential drugs using just minuscule amounts of chemical reagents.
Brian Cunningham and Charles Choi at the University of Illinois at Urbana-Champaign have designed a 96-well microplate that reduces the volume of precious chemicals needed to perform a drug screening assay.
This is no run of the mill microplate. Turn it over and you will see that its bottom surface is actually an elaborate network of fluid channels integrated with biosensors.
Microplates, flat plates with multiple wells used as tiny test tubes, are used in high-throughput screening (HTS). In HTS scientists screen though thousands of chemical compounds looking for an interaction with a target protein, which is a critical part of a disease process.
Detection of these biochemical interactions without the use of fluorescent labels is desirable as it can be tricky to add these labels in a reproducible way, and sometimes just impossible at all. Optical biosensors, like the photonic crystal ones used in this microplate, detect these interactions through the change in dielectric permittivity that occurs on the surface of the biosensor when molecules attach to it.Integrating biosensors with microfluidic channels allows the scientist to reduce the quantity of chemicals they use. However, not many biosensors are capable of interfacing with a large number of microfluidic channels in parallel, especially when the biosensors and fluid channels are small, said Cunningham.
In each 12-well row within the microplate, the fluid channels form 11 analyte wells. They are gathered to a single detection region, where all 11 channels can be monitored at once. A central common well in each row serves as an access point for introduction or withdraw of reagents for the flow channels.
They plan, said Cunningham, is to increase the level of integration so that a single three by five inch photonic crystal surface can support around 2500 microfluidic channels and assays.
Sarah Corcoran
A 96-well microplate incorporating a replica molded microfluidic network integrated with photonic crystal biosensors for high throughput kinetic biomolecular interaction analysis
Charles J. Choi and Brian T. Cunningham, Lab Chip, 2007
DOI: 10.1039/b618584c
Source: Royal Society of Chemistry
Posted under Discoveries, Innovations and Patents, HT Screening, North America, Press Releases | Comments Off
KU Medical Center to lead $7.5-million male contraceptive research and drug development program
Last Updated on Wednesday, 11 April 2007 10:50 Written by admin Wednesday, 11 April 2007 10:50
A researcher at the University of Kansas Medical Center has been awarded more than $7.5 million in funding from the National Institutes of Health to lead a team, including researchers at seven universities, in a collaborative effort to develop male contraceptives.
This five-year grant will establish the Interdisciplinary Center for Male Contraceptive Research and Drug Development, a multi-institutional organization that will work to develop new non-hormo¬nal, reversible male contraceptive agents for drug production.
The center will not only consist of research teams at KU Medical Center and KU-Lawrence, but also collaborators across the country at the University of Minnesota, Duke University, the University of California-San Fransisco, Robert Wood Johnson Medical School, and the University of Medicine and Dentistry of New Jersey. Funding for the center was awarded by the Contraception & Reproductive Health Branch of the National Institute of Child Health and Human Development.
The center will be directed by Joseph Tash, PhD, an associate professor of molecular and integrative physiology at KUMC, and associate director, Dr. Gunda Georg, Chair of Medicinal Chemistry at University of Minnesota. Tash, Georg, and a team of researchers at KUMC and KU Lawrence, have been conducting NIH-funded research, designing and testing male contraceptive agents, for more than five years.
Their work has lead to the development of some promising chemical compounds, such as Gamendazole, one of the most potent new oral anti-spermatogenic agents identified to date. Under this grant, research will continue on Gamendazole as well as exploring new lead compounds.
Tash said the group intends to take a multidisciplinary approach, focusing on several chemical compounds, and proteins that regulate testes function so that mature sperm are not produced. They are also concentrating on chemical agents that may temporarily deactivate enzymes so that sperm development is prevented or sperm are immobilized so the egg remains unfertilized. To identify new lead compounds, the center will utilize High Throughput Screening and proteomics to test hundreds of thousands of compounds.
While High Throughput Screening (HTS) technology is more common in private industry, KU is one of the few universities in the nation to have such a facility, which Tash said is important since many pharmaceutical companies have curtailed their research and development in male contraception. Without the HTS lab, screening hundreds of thousands of compounds could take years, but with the technology, screening time is dramatically reduced to weeks.
The research program in this center will go beyond identifying new protein targets involved in regulation of male fertility, and begin cutting edge drug discovery and design. The scientists involved in the research have a record of success in providing NIH with highly promising reversible non-hormonal male contraceptive agents.
Posted under Business and Investment, Grants and Awards, HT Screening, North America, Press Releases, Targeted Libraries | Comments Off
Advancing the Science of Drug Discovery: Bridging Research & Development
Last Updated on Thursday, 25 January 2007 08:49 Written by admin Thursday, 25 January 2007 08:49
Society for Biomolecular Sciences
Presents its 13th Annual Conference & Exhibition
Advancing the Science of Drug Discovery: Bridging Research & Development
April 15-19, 2007
Palais Des Congres de Montréal
Montréal, Canada
After the Society’s most successful annual event in Seattle this year, professionals from around the globe will want to participate in the next SBS Annual Conference & Exhibition in April 2007. This will be the first spring annual the Society has scheduled.
The SBS event, the premier scientific and showcase event in molecular discovery, brings together more than 2,900 professionals, offering a unique opportunity to learn more about the latest innovations, technologies, and research in the drug discovery sciences from all over the world. Session topics include:
· Advances in Screening Technologies
· Biomarkers: From Bench to Clinic
· Compound Management: Challenges & Automation Solutions
· Enzyme Targets: Black Box or Whole Cell Assays?
· From Gene to Target: Functional Target Validation Strategies
· High-Content Cellular Screening
· Immunotherapeutics, mAbs & Translational Medicine
· Structural Biology: Underpinning Drug Discovery
· Systems Biology & High-Throughput Approaches to Screening Native Cells
· Target Biology & Screening: GPCRs
· Target Biology & Screening: Ion Channels
· Toxicity Profiling Using High-Throughput & High-Content Technologies
Contact:
Marietta Manoni, CMP
Conference Manager
mmanoni@sbsonline.org
Society for Biomolecular Sciences
36 Tamarack Avenue, #348, Danbury, CT 06811, USA
Phone: +1 (203) 743-1336
Fax: +1 (203) 748-7557
Posted under HT Screening, Medicinal Chemistry, North America, Press Releases, USA and Canada | Comments Off
NEXUS Biosystems’ Universal Store Compound Management System Selected as Key Component of Vanderbilt University’s High-Throughput Screening Facility
Last Updated on Friday, 12 January 2007 11:05 Written by admin Friday, 12 January 2007 11:05
POWAY, CALIF., January 11 /CNW/ - NEXUS Biosystems announced that Vanderbilt University's High-Throughput Screening (HTS) Facility has selected the Universal Store to manage its ever-growing collection of synthetic small molecules and natural products. The Universal Store will serve as the main repository for maintaining and managing Vanderbilt's collection as a part of its basic research and translational drug discovery activities. Multiple local and extramural medicinal, synthetic, and natural products-based chemistry efforts contribute to the population of this collection. This collection is utilized in large part by the Vanderbilt Institute of Chemical Biology's (VICB) High-Throughput Screening (HTS) Facility. This facility utilizes state-of-the-art instrumentation and data management tools to interrogate chemical libraries, enabling identification of compounds and reagents for use in basic research, therapeutics, and diagnostics. The facility serves the Vanderbilt research community in developing and running HTS on a wide variety of targets using Vanderbilt's local chemical compound collection. In addition the facility exists as a national resource for screening G-protein coupled receptors (GPCRs), ion channels, and transporters as one of the ten-member, NIH-funded, Molecular Libraries Screening Center Network (MLSCN): http://mli.nih.gov/mlscn/index.php "We are very excited about the selection of our instruments as a major component of the VICB's on-going research initiative," stated Tommy Bui, VP of Business Development for NEXUS. "The VICB requires a sample management system that can achieve demanding requirements for performance, reliability, and most importantly, sample integrity. Vanderbilt's decision to implement the Universal Store further validates NEXUS' technology as a premier solution for the storage, retrieval, and management of diverse chemical libraries." Dave Weaver, Director of the Vanderbilt HTS Facility, said, "We are thrilled to be working with NEXUS to deploy its compound storage and management system. We extensively evaluated numerous compound management systems and we particularly prized the Universal Store's flexibility, scalability, and functionality. For us, getting a system that was able to serve our present needs while being built on a design philosophy that ensures its ability to accommodate future advancements in compound storage was extremely appealing." About NEXUS Biosystems, Inc. NEXUS Biosystems, a privately held company based in Poway, California, USA, has since 1996 been a developer and provider of enabling technologies and automation systems for pharmaceutical, biotech, agrochemical, and academic research institutions worldwide. Current products include the Universal Store(R) family of next-generation sample storage and retrieval systems, the Crystal Farm(R) line of protein crystallization systems, the IRORI(R) line of chemical synthesis technologies and services, and in No. America and Asia NEXUS is a distributor of the Covaris(TM) line of ultrasonic products for sample dissolution, resolubulization, and high density microplate mixing. About the Vanderbilt Institute of Chemical Biology The Vanderbilt Institute of Chemical Biology is a trans-institutional initiative between the College of Arts and Sciences and the School of Medicine. The Institute's mission is to provide research and training in the application of chemical approaches to the solution of important biomedical problems. The proximity of the Chemistry Department and the School of Medicine facilitates this process. Our members represent a range of research interests and technologies with particular strengths in analytical methodology and molecular imaging, cellular responses to chemical stress, drug discovery, enzyme and receptor chemistry, proteomics, structural biology, and chemical synthesis.
For further information: NEXUS Biosystems Tommy Bui, VP, Business Development (858) 679-0770
Posted under Equipment & Supplies, HT Screening, North America, Press Releases | Comments Off
Compatibility of Cell-Based Assays with High-Throughput Screening Proving to Be a Key Challenge
Last Updated on Wednesday, 6 December 2006 08:15 Written by admin Wednesday, 6 December 2006 08:15
DUBLIN, Ireland–(BUSINESS WIRE)–Research and Markets has announced the addition of “Development of Cell-Based Assays (Technical Insights)†to their offering.
This Frost & Sullivan research service titled Developments in Cell Based Assays focuses on the technological advancements, emerging trends, drivers, and challenges affecting the development of cell-based assays. The research service provides information on major companies and academic institutions involved in the development of innovative technology and products. A summary of key patents gives an insight into notable activities, technology trends, and important participants in this field.
Market Sectors
Expert Frost & Sullivan analysts thoroughly examine the following market sectors in this research:
- Healthcare – Drug Discovery
Technologies
The following technologies are covered in this research:
- High Throughput
- Multiplexing
Market Overview
Compatibility of Cell-based Assays with High-throughput Screening Proving to be a Key Challenge
The ability to generate significant time and cost savings is pushing many pharmaceutical and biotechnology companies to favour cell-based assays over other methods such as biochemical and in-vitro assays. Cell-based assays are finding numerous applications in target identification and validation, monitoring cellular events, as well as the screening compounds for efficacy and biosafety. Researchers now face the challenge of ensuring greater compatibility with high-throughput screening (HTS), which is emerging as one of the most sought-after technologies to perform cell-based assays. HTS provides ideal support for cell-based assays by not only increasing the number of analyzed samples, but also offering high-quality information. Used in combination with HTS, cell-based assays offer greater quantity of data coupled with superior-quality data assays, leads, screening process, and compound libraries, explains the analyst of this research service.
Going forward, the focus is expected to be on easy-to-use and highly sensitive assays that provide continuous records of cellular activity. Although, most research activities currently concentrate on drug discovery, cell-based assays are expected to gain popularity in diagnostics, molecular biology, biochemistry and neuroscience, genetics, toxicology studies, bioengineering, and proteomics, among other fields as they become more cost-effective and biologically significant.
Focus on Developing Robust and Reliable Cell-based Assays
The increasing demand for higher-quality output, healthier consistent cells, and improved assay data in drug discovery is leading researchers to focus on developing robust and highly reliable assays through the automation of well-characterized cell lines. The automation of cellular assays is also likely to improve the drug discovery process by identifying the right leads and by understanding their chemistry more accurately. Although the automation of cell-based assays is expected to be a hugely popular trend, the key is to ensure strict environment control due to the involvement of live cells. For example, automated incubators store stacks of microplates at a controlled temperature and humidity.
Miniaturization is another step toward more-efficient cell-based assays. Recent advances in assay chemistries and signal detection technology allow the miniaturization of cell-based assays, making it convenient to perform dose-response experiments during primary screens. Simpler and faster screening is also possible though the use of homogenous assay techniques for radioactive, fluorescent, and luminescent assay formats. Homogenous assay formats are user-friendly and also minimize errors by allowing the direct use of cell samples or lysine and other reagents, without having to purify or separate them before taking measurements, says the analyst.
For more information visit http://www.researchandmarkets.com/reports/c46516
Posted under Europe, HT Screening, Press Releases | Comments Off
BioTrove Screens Two Million Samples Using RapidFire Lead Discovery, a Label Free High-Throughput Mass Spectrometry Platform for Intractable Drug Targets; Four Clients to Present Data at Upcoming Society for Biological Sciences Meeting
Last Updated on Thursday, 5 October 2006 03:18 Written by admin Thursday, 5 October 2006 03:18
WOBURN, Mass.–(BUSINESS WIRE)–Sep 12, 2006 – BioTrove, Inc. announced today the successful screening of more than two million individual samples using their RapidFire(TM) Lead Discovery System. RapidFire(TM) is a unique, mass spectrometry-based, high-throughput screening platform that facilitates label-free screening of challenging drug targets using native substrates.
BioTrove currently provides screening services and instrumentation to nine large pharmaceutical and biotechnology companies. Four of these clients will present results of lead discovery campaigns at the upcoming Society for Biomolecular Sciences (SBS) conference (Seattle, WA, September 17-21), demonstrating RapidFire(TM) screening of previously intractable drug targets.
RapidFire(TM) Lead Discovery uses mass spectrometry to enable high throughput screening of functional biochemical assays via label-free analysis of native substrates. The unique platform can analyze individual assays at throughputs of four to eight seconds per sample–a dramatic increase in throughput over conventional liquid chromatography-mass spectrometry systems.
BioTrove offers access to the Lead Discovery System as a screening service that includes assay development, primary screening, and support of secondary screening and chemistry programs. Technology transfer is available for clients who prefer to own their systems.
“We feel that the addition of six new customers in the past year, along with the screening of our two millionth client sample, truly validates the ability of the RapidFire(TM) platform to unlock the potential of a wide range of challenging HTS targets,” said Can (Jon) Oezbal, Ph.D., Director of the RapidFire(TM) program. “The RapidFire(TM) system has now been used to identify lead compounds in a wide range of high-throughput screening projects, ranging from key metabolic disease, cardiovascular, and oncology targets to novel targets in the anti-infective and anti-fungal areas.”
Presentations will be made at the upcoming SBS meeting by BioTrove’s RapidFire(TM) clients from Bayer Pharmaceuticals, Pfizer Inc., Schering Plough Research Institute, and Sirtris Pharmaceuticals. BioTrove will also exhibit at SBS, at booth number 636.
About BioTrove, Inc.
BioTrove offers two innovative platform technologies that dramatically increase the throughput of pharmaceutical screening and SNP genotyping.
RapidFire(TM) Lead Discovery enables difficult targets (lipids, fatty acids, phospholipids, steroids, prostaglandins, and others) to be screened using a high-throughput, native detection method (high throughput mass spectrometry) in less than eight seconds per sample.
OpenArray(TM) enables genomics researchers to generate up to hundreds of thousands of SNP data points per day. The flexible format and nanoliter scale of the OpenArray(TM) system allows adjustment of sample and assay numbers, for economical high-throughput genotyping.
Contact BioTrove, Inc. Selena Larkin, Ph.D., 571-451-4389 slarkin@biotrove.com or Feinstein Kean Healthcare Courtney Harris, 617-761-6744 courtney.harris@fkhealth.com
Posted under HT Screening, North America, Press Releases, Targeted Libraries | Comments Off
Frost & Sullivan Recognizes DiscoveRx’s Innovative Assay Technology for Drug Screening and Overall Achievements in Intact Cell-Based Assays
Last Updated on Thursday, 5 October 2006 02:42 Written by admin Thursday, 5 October 2006 02:42
PALO ALTO, Calif., Sept. 7 /PRNewswire/ — Frost & Sullivan selected DiscoveRx Corp. as the recipient of the 2006 Frost & Sullivan Award for Technology Innovation for its development of the PathHunter(TM), an innovative protein trafficking platform technology. In its simplest format, this assay system allows users to monitor signaling pathways using translocation in whole cells. Today, DiscoveRx offers a broad range of assays and services for evaluating compound effects on various cellular pathways including their most recent addition, PathHunter Beta-Arrestin assays for GPCR activation.
PathHunter is based on the DiscoveRx’s proprietary technology platform: Enzyme Fragment Complementation (EFC) technology. EFC has been used to develop a series of highly validated biochemical HTS assays for GPCR, Kinases and Proteases. PathHunter is a modification of this highly versatile platform into a cell based format. PathHunter represents the first chemiluminescence assay technology that can measure protein trafficking directly inside the cell and act as a liaison between in vitro biochemical assays and the more complex multiparameter imaging technologies.
“Screening technologies that are faster, more cost effective and that provide biological rich information are always sought after,” says Frost & Sullivan Research Analyst R. Srimathy. “PathHunter offers several benefits that position it to be the assay technology of choice.”
For instance, it allows the user to reduce the complexity of using cell- based assay to simple microtiter plate formats. PathHunter assays (as well as HitHunter assays) are homogeneous in nature, one- or two-step reagent addition assays, which do not need any cell washing or cell fixation steps.
Furthermore, the assays are compatible with many different cell types and especially suited for cell types most commonly used in high throughput screening (HTS) settings (Chinese Hamster Ovary [CHO], Human Embryonic Kidney [HEK]).
Some of the main advantages of DiscoveRx’s technology for cell-based assays are increased throughput in 384 well formats, compatibility with luminescent plate readers, and delivery of luminescence output for reduced interference from fluorescent compounds.
The PathHunter is also readily adaptable to automated screening and performs novel HTS assay for new classes of compounds. It has a simplified method for sample preparation and offers a wide range of assays such as translocation, degradation, secretion protein: protein interaction and membrane trafficking.
The PathHunter platform allows scientists to detect protein trafficking without any form of imaging features and it is highly cost effective, that is, the cost involved is only a fraction of the cost involved in using the normal green fluorescent protein (GFP)-based assays. Furthermore, the technology can also be miniaturized and used for 1536 format.
“DiscoveRx is being increasingly recognized in the pharmaceutical and biotechnology sector for creating advanced assays for G protein-coupled receptors (GPCRs), kinases, and other drug target classes,” notes Srimathy. “The company’s in vitro biochemical and cell-based assays will help accelerate drug discovery and development even as the PathHunter technology is being used to look at other protein movement.”
In summary, the Frost & Sullivan Award for Technology Innovation recognizes DiscoveRx for its introduction of an innovative technology platform, the PathHunter, and its overall work on intact or lysed cell-based assays for GPCR, kinases, proteases, and nuclear hormone receptors.
Each year Frost & Sullivan presents this Award to a company that has demonstrated and carried out new research, which has resulted in innovation(s) that have or are expected to bring significant contributions to the industry in terms of adoption, change, and competitive posture. This Award recognizes the quality and depth of a company’s research and development program as well as the vision and risk-taking that enabled it to undertake such an endeavor.
Frost & Sullivan Best Practices Awards recognize companies in a variety of regional and global markets for demonstrating outstanding achievement and superior performance in areas such as leadership, technological innovation, customer service, and strategic product development. Industry analysts compare market participants and measure performance through in-depth interviews, analysis, and extensive secondary research in order to identify best practices in the industry.
About DiscoveRx Inc.
Founded in 2000, DiscoveRx is a privately held, venture-backed company headquartered in Fremont, California, with an additional office in Birmingham, England. The Company pioneered the use of Beta-galactosidase enzyme fragment complementation in biochemical and cell based assays for discovery research, and holds extensive intellectual property in this area. DiscoveRx is dedicated to the development and commercialization of innovative solutions to study GPCRs, Kinases and other major drug target classes, and many of their innovative products have been widely adopted in pharmaceutical and biotech drug screening laboratories worldwide. For more information on DiscoveRx products, please visit http://www.discoverx.com
Contact: Ms. Sailaja Kuchibhatla 1-510-979-1415 ext.104 (skuchibhatla@discoverx.com) About Frost & Sullivan
Frost & Sullivan, a global growth consulting company, has been partnering with clients to support the development of innovative strategies for more than 40 years. The company’s industry expertise integrates growth consulting, growth partnership services, and corporate management training to identify and develop opportunities. Frost & Sullivan serves an extensive clientele that includes Global 1000 companies, emerging companies, and the investment community by providing comprehensive industry coverage that reflects a unique global perspective and combines ongoing analysis of markets, technologies, econometrics, and demographics. For more information, visit http://www.awards.frost.com or http://www.drugdiscovery.frost.com .
Contact: Stacie Jones 210.247.2450 Stacie.jones@frost.com
Posted under Grants and Awards, HT Screening, North America, Press Releases, Targeted Libraries | Comments Off
Discover the Latest Improvements to Compound Screening In Pharmaceutical Research and Chemical Biology – Throughput Screening in Drug Discovery
Last Updated on Thursday, 5 October 2006 02:39 Written by admin Thursday, 5 October 2006 02:39
DUBLIN, Ireland–(BUSINESS WIRE)–Sep 19, 2006 – Research and Markets (http://www.researchandmarkets.com/reports/c42217) has announced the addition of High-Throughput Screening in Drug Discovery to their offering.
This book is designed as a professional guide for successful compound screening in pharmaceutical research and chemical biology. It discusses the rationale behind successful and “intelligent” screening approaches and presents current methods and technologies for assaying bioactive molecules in a high-throughput situation. In addition, it treats in detail the analysis of the date generated in the assay and chemoinformatics support for high-throughput data management – a facet that is often neglected but is of tremendous practical importance. With its focus on bioanalysis and chemical biology, the book will be part of our rapidly growing cluster in this area.
Discover the latest improvements to compound screening in pharmaceutical research and chemical biology, including the chemoinformatic tools needed for proper data evaluation. With contributions from leading pharmaceutical companies in Europe and the US.
Contents Include:
Chemical Genetics (C. Shamu, Harvard University)
High-Throughput Screening for Targeted Drug Discovery (J. Huser, Bayer Healthcare)
Laboratory Automation (J. Comley, Cambridge, UK)
Binding Assays (L. Mayr, Novartis Pharma)
Cell-based Assays (S. Rees, GlaxoSmithKline)
Biochemical Assays (W. Mallender, Millennium Pharmaceuticals)
High-Content Screening (P. Lipp, University of Homburg/Saar)
Handling and Management of Primary Assay Data (H. Gubler, Novartis Pharma)
Chemoinformatic Tools for HTS Data Analysis (S. Mundt, Bayer HealthCare)
Efficient Use of Compound Libraries: Random Screening vs. Focused Libraries (M. Beck, Bayer CropScience)
Data Mining Using Cell-Based Assay Results (J. Caldwell, Novartis Institute)
For more information visit http://www.researchandmarkets.com/reports/c42217
Contact Research and Markets Laura Wood press@researchandmarkets.com Fax: +353 1 4100 980
Posted under Europe, HT Screening, Press Releases | Comments Off
Institut Pasteur Korea Selects ActivityBaseâ„¢ as its Screening Solution of Choice
Last Updated on Thursday, 5 October 2006 02:37 Written by admin Thursday, 5 October 2006 02:37
IDBS has announced that Institut Pasteur – Korea has implemented the ActivityBase data management software suite to increase efficiency and throughput in its screening operations.
Institut Pasteur Korea (IP-K), a Research Center located in Seoul, South Korea, has purchased ActivityBase to handle their biology and chemistry data for High Throughput and High Content Screening (HTS/HCS).
IP-K is implementing HCS assays and platforms for Drug Discovery using cell-based models of disease and automated confocal microscopy.
IP-K will use ActivityBase suite to consolidate chemistry information and screening results, including those from microscopy-based screens, in a single Oracle database.
Institut Pasteur Korea decided to purchase ActivityBase as its researchers felt more secure with a system with a proven track record in Drug Discovery.
Dr. Thierry Christophe, the Head of the Screening and Pharmacology lab, has used ActivityBase in previous positions at other companies.
He said, “I am happy to be working with ActivityBase again, as it is a robust and flexible system that I know can deliver the results we need.”
“We plan to develop specific data analysis templates for High Content Screens allowing the manipulation of multiplexing data from one single screen.”
Neil Kipling, IDBS’ Chairman and CEO, commented, “The increase in HCS and HTS planned by IP-K’s screening group demanded a data management system that could scale up to their requirements, both now and in the future, as well as map closely to their workflow.”
“We are delighted to be supporting a centre of excellence in biomedical research and technology development, allowing new drugs to be identified faster and more reliably.”
Further Information: http://www.ip-korea.org
Posted under Asia, ChemInformatics, HT Screening, Press Releases | Comments Off
EpiCept Announces IND Filing of Novel Compound with Potent Apoptotic and Tumor Selective Vascular Disruptive Activity for Treatment of Cancer
Last Updated on Thursday, 5 October 2006 02:20 Written by admin Thursday, 5 October 2006 02:20
NGLEWOOD CLIFFS, New Jersey, October 2 /PRNewswire/ – – EPC2407 Latest Clinical Candidate from Company’s Apoptosis ScreeningTechnology EpiCept Corporation (Nasdaq: EPCT; OMX Stockholm) today announced that ithas submitted an investigational new drug (IND) application to the U.S. Foodand Drug Administration (FDA) to begin Phase I clinical studies of EPC2407 incancer patients. EPC2407 is the Company’s novel small molecule which inducesapoptosis (cell death) and disruption of tumor blood flow. EPC2407 isintended for the treatment of advanced cancer patients with solid tumors thatare well vascularized. These tumors include the frequently occurring cancersof the lung, ovaries, and breast. These cancers still have a high mortalityrate despite progress in earlier stages of these diseases. (Logo: http://www.newscom.com/cgi-bin/prnh/20020513/NYM112LOGO ) EPC2407 is the first of a new class of microtubulin inhibitors whichcause cell cycle arrest, caspase activation and apoptotic death in cancercells. The compound has demonstrated in pre-clinical studies potentanti-tumor activity against a number of tumor types and is synergistic withcisplatin. EPC2407 also disrupts the vasculature of tumor blood vesselsleading to hypoxia and tumor necrosis. This has been shown to occur inpre-clinical studies in tumored animals at subtoxic concentrations. Theobjectives of this first clinical trial of EPC2407 is to determine themaximum tolerated dose, to characterize the blood levels and biologicaleffects of the drug and to identify any anti-tumor response as measured by CTscans, MRI or PET scans. The study is expected to enroll approximately 30-40patients. One of the investigators for this study is Dr. Daniel von Hoff from theCenter for Translational Drug Development, TGen, the Scottsdale HealthcareClinical Research Institute and the Arizona Cancer Center. Dr. von Hoffcommented, “We are pleased to work with EpiCept Corporation to test thispotential new anti-cancer compound in patients with advanced cancers. Resultsfrom pre-clinical testing of EPC2407 are encouraging, and mechanism studiessuggest two ways that this new agent may add to our treatment options for arange of cancers.”“The filing of an IND for EPC2407 represents an important milestone forour company,” stated Jack Talley, President and Chief Executive Officer. “Webelieve this filing deepens our already promising clinical pipeline of painand cancer treatment candidates and further demonstrates the potential of ourproprietary apoptosis screening technology which led to the discovery anddevelopment of EPC2407. This compound represents the second clinical cancercandidate discovered by EpiCept researchers utilizing this technology. Wehave identified several other promising compounds with the potential forfurther development which we intend to selectively pursue. Our goal is toprogress these product candidates into clinical development and seek partnersprior to the commencement of pivotal scale trials.” About EPC2407 The IND filing for EPC2407 is based on the compound’s effectiveness inseveral pre-clinical animal models of cancer and its potent anti-tumoreffects both in vitro and in vivo. Nanomolar concentrations of the moleculehave been shown to induce tumor cell apoptosis and to selectively inhibitgrowth of proliferating cell lines, including multi-drug resistant celllines. Murine models of human tumor xenografts demonstrated that EPC2407inhibits growth of established tumors of a number of different cancer types.The safety profile of the compound in standard toxicology studies alsosupports its testing in human clinical trials. Pre-clinical studies suggest that the anti-tumor effects of EPC2407 maybe the result of a dual mechanism, a direct effect of tumor apoptosis and asecond effect on disruption of tumor vascular endothelial cells leading tohypoxia and central tumor necrosis, as observed with vascular disruptionagents. About EpiCept’s Apoptosis Screening Technology Cancer cells often exhibit unchecked growth caused by the disabled orabsent natural process of programmed cell death called apoptosis. Apoptosisis a normal process of triggering destruction of cells from within when theyhave outlived their purpose or may be seriously damaged, but cancer cellsgrow out of control when the normal apoptosis process is not functioning. Apromising approach in the fight against cancer is selective induction of orrestoration of apoptosis, thereby checking, and perhaps reversing, theimproper cell growth. EpiCept’s proprietary apoptosis screening technology can efficientlyidentify new cancer drug candidates and molecular targets that selectivelyinduce apoptosis in cancer cells through the use of chemical genetics and itsproprietary live cell high-throughput caspase-3 screening technology.Chemical genetics is a research approach investigating the effect of smallmolecule drug candidates based on the cellular activity of a protein,enabling researchers to determine the protein’s function. With thecombination of chemical genetics and caspase-3 screening, EpiCept’sresearchers identify and test the effect of small molecules on pathways andmolecular targets crucial to apoptosis and gain insights into their potentialas new anticancer agents. The Company’s screening technology is particularlyversatile and can be adapted for many cell types that can be cultured, and itcan measure caspase activation inside multiple cell types (e.g. cancer cells,immune cells, or cell lines from different organ systems or geneticallyengineered cells). This allows researchers to find potential drug candidatesthat are selective for specific cancer types, which may help identifycandidates that provide increased therapeutic benefit and reduced toxicity. EpiCept’s drug discovery and pre-clinical development groups include highthroughput screening (HTS) and informatics, cell biology, medicinalchemistry, and in vivo pharmacology. The HTS group identifies the hits whichupon passing certain criteria are analoged by the chemistry group forsecondary and tertiary assay testing by the cell biology group. Promisingleads are tested in animal models for toxicity, efficacy andpharmacokinetics. An iterative interaction between the various groupsprovides for the rapid advancement from hit compounds to lead candidatessuitable for further development. About EpiCept Corporation EpiCept is an emerging specialty pharmaceutical company focused on unmetneeds in the treatment of pain and cancer. The Company has a staged portfolioof product candidates with several pain therapies in late-stage clinicaltrials, and a lead oncology compound (for acute myeloid leukemia, AML) withdemonstrated efficacy in a Phase III trial; a marketing authorizationapplication for this compound will be submitted in Europe in the near future.EpiCept is based in New Jersey, and the Company’s research and developmentteam in San Diego is pursuing a drug discovery program focused on novelapproaches to apoptosis. Forward-Looking Statements This news release contains certain forward-looking statements thatinvolve risks and uncertainties that could cause actual results to bematerially different from historical results or from any future resultsexpressed or implied by such forward-looking statements. Such forward-lookingstatements include statements regarding the efficacy, safety, and intendedutilization of the Company’s product candidates, the conduct and results offuture clinical trials, the sufficiency of the Company’s existing capitalresources, plans regarding regulatory filings, future research and clinicaltrials and plans regarding partnering activities. Factors that may causeactual results to differ materially include the risk that product candidatesthat appeared promising in early research and clinical trials do notdemonstrate safety and/or efficacy in larger-scale or later stage clinicaltrials, the risk that the Company will not obtain approval to market itsproduct candidates, the risks associated with reliance on outside financingto meet capital requirements, and the risks associated with reliance oncollaborative partners for further clinical trials, development andcommercialization of product candidates. You are urged to consider statementsthat include the words “may,”"will,”"would,”"could,”"should,”"believes,”"estimates,”"projects,”"potential,”"expects,”"plans,”"anticipates,”"intends,”"continues,”"forecast,”"designed,”"goal,” or the negative ofthose words or other comparable words to be uncertain and forward-looking.These factors and others are more fully discussed in the Company’s periodicreports and other filings with the SEC. EPCT-GEN Web site: http://www.epicept.comEpiCept CorporationRobert W. Cook, EpiCept Corporation, +1-201-894-8980, rcook@epicept.com; or Francesca T. DeVellis, Feinstein Kean Healthcare, +1-617-577-8110, francesca.devellis@fkhealth.com /Photo: http://www.newscom.com/cgi-bin/prnh/20020513/NYM112LOGO
Posted under Drug-Like Compounds, Europe, HT Screening, North America, Press Releases | Comments Off
AnaSpec Develops Industry’s Only HTS Assay Kits for Screening HCV NS3/4A
Last Updated on Tuesday, 18 July 2006 01:41 Written by admin Tuesday, 18 July 2006 01:41
San Jose, CA – July 6, 2006
Hepatitis C virus (HCV), belonging to the Flaviviridae family of positive, single stranded RNA, infects approximately 170 million people worldwide (1). The HCV polyprotein consists of structural proteins (C, E1, E2 and p7), and the non-structural (NS) proteins (NS2, NS3, NS4A, NS4B, NS5A, and NS5B) as a result of proteolytical cleavages of host signal peptidases; and metalloprotease and serine proteases, respectively.Â
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AnaSpec has developed the industry’s only HTS assay kits for screening HCV NS3/4a. EnzoLyteTM assay kits are specifically designed for the detection and quantification of NS3/4A protease activity at subnanomolar concentrations. They can be used in 96- or 384-well microplate format. There are three assay kits to choose from depending on what wavelength is used for monitoring the cleavage of the FRET substrate. Convenient mix-and-read format and one-step procedure make EnzoLyte Assay Kits ideal for high-throughput screening.
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Peptide substrate paired with Dabcyl (fluorophore) and Edans (quencher). Fluorescence can be continuously monitored at Ex/Em=340/490nm. Kit size: 500 assays.
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Peptide substrate paired with 5-FAM (fluorophore) and QXLTM 520 (quencher). Fluorescence can be continuously monitored at Ex/Em=490/520 nm. Kit size: 100 assays.
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Peptide substrate paired with HiLyte FluorTM TR (fluorophore) and QXLTM 610 (quencher). With near red emission wavelength, this FRET peptide avoids the autofluorescence interference associated with most test compounds. Fluorescence can be continuously monitored at Ex/Em=590/620nm. Kit size: 100 assays.
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References:
1. CDC and Prevention. Morb. Mortal. Wkly. Rep. 47:1-39 (1998).
Posted under HT Screening, New Products, North America, Press Releases | Comments Off
ODYSSEY THERA GRANTED U.S. PATENT FOR PATHWAY-BASED DRUG DISCOVERY STRATEGY
Last Updated on Monday, 3 July 2006 08:49 Written by admin Monday, 3 July 2006 08:49
Ninth Patent for PCA Broadly Covers Assay and Screening Technologies
San Ramon, California, June 20, 2006 – Odyssey Thera, Inc. announced today that the United States Patent and Trademark Office granted U.S. Patent No. 7,062,219 for single- and multi-color protein-fragment complementation assays (PCA) in drug discovery.
The patent provides methods for constructing diverse assays in live cells for detecting dynamic changes in protein complexes and pathways. Additional methods describe application of these assays to automated, high throughput and high content screening. Broad claims cover the construction of assays on known and unknown pathways, using a wide array of reporter systems, expression strategies and assay formats.
“This patent describes a unique and flexible strategy for drug discovery†said John K. Westwick, Ph.D., patent co-author and Odyssey Thera President and CSO. “The strategy achieves three key goals: first, a massive increase in the scope of cell-based, biologically relevant screens for drug discovery and profiling. Importantly, the claims are not limited to particular targets, cell types or assay formats, and we’ve constructed assays for all major target classes. Second, we describe how these tools are applied to high throughput drug discovery, enabling the screening of large compound libraries. Finally, we demonstrate that the assays accurately reflect the activity of drug targets in their native context, resulting in screening hits of greater quality and likelihood of successâ€.
Professor Stephen Michnick of the University of Montreal, PCA inventor and co-author on the patent, added “I originally set out to address the need for a universal approach to study the dynamics of biochemical pathways. That it could also be used to decipher drug actions on signaling pathways was implicitly understood, but I am gratified that this patent and our recent publications demonstrate the practical realization of how this technology can be broadly applied to improve pharmaceutical R&Dâ€.
This patent adds to over forty issued patents and pending applications covering broad aspects of pathway-based discovery technologies, and solidifies Odyssey Thera’s leadership position in these fields.
About Odyssey Thera
Odyssey Thera, Inc. is a privately held biotechnology company that is pioneering a pathway-based approach to drug discovery. The use of human cells instead of isolated proteins aids in the identification of drug leads with desirable profiles, and enables early attrition of compounds with unintended effects in human cells. The company is applying its strategy both for the benefit of its pharmaceutical partners, and to identify small molecules that block key cancer pathways in man. Visit Odyssey Thera’s website at http://www.odysseythera.com
Posted under Discoveries, Innovations and Patents, HT Screening | Comments Off
In silico innovation for optimal drug candidates
Last Updated on Monday, 19 June 2006 06:57 Written by admin Monday, 19 June 2006 06:57
Chimatica describes itself as a unique drug design and discovery contract research organisation. Using virtual screening and informatics methods, the Chimatica approach significantly reduces costs and timescales by providing drug candidates with the highest possible chance of success. Industry-leading methods for receptor docking and simulation are used to select structure-based drug design targets for laboratory testing, and large-scale pharmacophore searching and Qsar analysis are used to identify ligand-based targets.
Chimatica provides access to commercially available, proprietary and virtual chemical databases on the multi million-compound scale with predefined drug characteristics.
Virtual design is used to access new compounds and create bespoke virtual libraries that allow access to new and better high calibre drug candidates for a wider range of disease.
Through the combination of industry-recognised expertise, state of the art software and proprietary large-scale computing infrastructure, the company’s advanced in silico capabilities in molecular design and simulation provide the most effective path to drug innovation.
From fully outsourced projects or working co-operatively with in-house teams, Chimatica helps bridge the gap between disease targets and optimal quality drug candidates with significantly lower costs and increased potential revenues.
Posted under ChemInformatics, Europe, HT Screening, Press Releases | Comments Off
Ingenium and ASINEX Announce Successful Lead Optimization Program
Last Updated on Wednesday, 7 June 2006 06:04 Written by admin Wednesday, 7 June 2006 06:04
MUNICH and MOSCOW, June 6 /PRNewswire/ — Ingenium Pharmaceuticals AG, a drug discovery and development company, and ASINEX Ltd., a leading provider of lead generation and chemical optimization services, announced today a successful lead optimization project resulting in the generation of novel active compounds, which will expand Ingenium’s current proprietary pipeline of potential treatments for pain and inflammatory diseases. Due to the success of this completed project, the two companies will continue the collaboration throughout 2006.
Commenting on the agreement, Dr. Klaus Dembowsky, Ingenium’s Vice President of Drug Discovery, said, “As Ingenium continues to advance its drug discovery and development programs through preclinical pharmacological evaluation, effective lead optimization is critical. ASINEX has performed rapidly and efficiently to meet our needs and we have filed key patents based on these novel compounds.”
“We are looking forward to continuing our collaboration with Ingenium. After starting on a small scale, our relationship has grown over the last few months. We have successfully completed challenging tasks for Ingenium, and we are delighted that our work has made a positive impact on the company’s pipeline,” said Dr. Andrea Altieri, ASINEX’s Head of Project Management.
Posted under Drug-Like Compounds, HT Screening, Press Releases | Comments Off
Advancing Drug Discovery: From Better Hits to Better Candidates
Last Updated on Wednesday, 7 June 2006 05:59 Written by admin Wednesday, 7 June 2006 05:59
SBS 12th Annual Conference and Exhibition
September 17-21, 2006 – Seattle, WA, USA
The theme of the SBS 2006 annual conference in Seattle highlights the impact of screening and technology applications on drug discovery. With over a decade of HTS and combinatorial chemistry strategies now behind us, it is important to understand and critique the impact these technologies have had on providing better hits, better leads and most of all, better drug candidates to ultimately improve the quality of patient care.
Technical Session Summaries
No matter what part of the drug-discovery process you’re involved in, you’ll find plenty to interest you in the 2006 SBS Technical Sessions. This professional program presents issues and information from the best minds in the industry—covering the latest developments at every stage of the process and in every area of drug discovery.
With an unparalleled professional program comprising more than 45 presentations, you’ll get useful information and valuable insights to take back to your lab or workplace.
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Advanced Technology for Drug Discovery
Session Chairs:
Scott Diamond, University of Pennsylvania, USA
David Weaver, Vanderbilt University, USA
HTS labs are now conducting a continually increasing number of assays per year and are also encountering more difficult and nontraditional assays. This session will focus on emerging platforms and detection systems relevant to high-throughput screening challenges, including flow cytometry based HTS, microfluidics, microsensing, chemical microarrays, and label-free detection using mass spectrometry. Attendees of this session will learn how experts in the field are applying new technologies for challenging applications.
Target Biology & Screening sponsored by
Gary Krishnan, Eli Lilly, USA
Peter Lander, Eli Lilly, USA
Many companies have established platform approaches to identify novel leads and drug candidates for protein families or classes such as GPCRs, enzymes and ion channels. These efforts have addressed target biology and screening and have presented exciting opportunities to address therapeutic opportunities. These platform approaches have enabled high-throughput assays that optimally address target biology and selectivity and seize synergies among the individual projects in the same target class. This session will focus on the application of novel and traditional approaches used to produce better leads and candidates that target the biology of these important target classes.
Cells & Protein Production: Keeping Pace with Drug Discovery
Session Chairs:
Tom Kost, GlaxoSmithKline, USA
Lorenz Mayr, Novartis Pharma AG, Switzerland
The timely development, production and supply of high quality protein and cell-based reagents for HTS and compound profiling assays present a continual challenge within drug-discovery programs in both Pharma and Biotech. In addition to validating that a large number of diverse reagents possess the desired biological properties, one often needs to consider biosafety, stability, delivery, storage and tracking requirements. These requirements take on increased importance in the framework of the dramatic increase in the number of screening assays being performed in automated facilities that may be carried out by different groups in geographically distinct locations. Furthermore, recent trends in industry towards targets with less target validation and detailed knowledge about target production, demand continual enhancements of reagent production technologies. Attendees will learn of current approaches and future challenges of keeping pace with the supply of biologically relevant proteins, membranes, viruses and cells required to conduct productive drug-discovery programs.
Creating New Chemical Space for Lead Discovery
Session Chairs:
Michael Sofia, Pharmassett, Inc., USA
Armen Boldi, Discovery Partners International, USA
The objective of lead discovery is to identify a series of chemotypes that can be further progressed into expanded lead optimization. The primary strategies that are employed to support lead generation include high-throughput screening, focused screening, and structure-based approaches. All of these approaches require access to novel and diverse sets of compounds from either natural or synthetic sources that can be evaluated against the biological target of interest. The development of the necessary chemical space to support productive lead generation has spawned new approaches in the areas of natural products and synthetic natural product-like molecules, the evolution of high-throughput chemistry, the application of lead-like versus drug-like concepts, and the development of fragment-based strategies. It has also led to significant efforts to understand the interface between chemical and biological space and what characteristics are important in making a collection of compounds productive for lead generation. This session will address current chemical and theoretical approaches that are being employed to ensure that lead discovery efforts are providing quality leads to support down stream lead optimization needs.
Defining Target & Compound Specificity
Session Chairs:
William Janzen, Amphora Discovery Corporation, USA
Doriano Fabbro, Novartis Institute for Biomedical Research, Switzerland
Target specificity can mean many different things. Protein families such as protein kinases, GPCRs and ion channels play an essential role in many signaling pathways, and have, therefore, the potential to contribute to diseases ranging from cancer, inflammation and diabetes to cardiovascular and infectious disorders. Specificity as it is related to disease involvement is key to defining druggable targets, but identification of specific interactions and functional validation of targets remains a challenge. This session will explore contextual usage of the term specificity as well as methods for exploring compound target interactions and innovative approaches that have been developed to address specificity.
Hit to Lead Processes
Session Chairs:
Michael Sofia, Pharmasett, Inc., USA
Raju Mohan, Exelixis, Inc., USA
Prior to committing significant lead optimization resources to a HTS, active extensive validation of the chemotype is required. Therefore, the “hit to lead†process has evolved as a distinct phase in medicinal chemistry, bridging the gap between lead generation and full medicinal chemistry lead optimization. This process typically entails assessment of the pool of screening actives, validation of progressible SAR within selected chemical series, an early understanding of potential toxicological or metabolic liabilities, a clear understanding of IP and freedom-to-operate scope, and demonstration of in vitro potency and early indications of in vivo efficacy where possible. New cheminformatics tools, high-throughput assays that support liability assessment and the application of rapid analoging to scope out SAR trends are only a few of the emerging technologies utilized in critical decision making in the hit-to-lead phase. This session will highlight real examples of hit to lead development and showcase the application of novel approaches and tools that help accelerate the process.
Imaging & High Content Assays
Session Chairs:
Tina Garyantes, Sanofi-Aventis, USA
Renata Schnitzer, Boehringer Ingelheim, Austria
As the pharmaceutical industry struggles to increase productivity, there is a move toward using more physiologically relevant cellular assays and acute in vivo models earlier in the drug-discovery process. Examples include the re-emergence of phenotypic screening, the use of translocation assays for GPCRs and tyrosine kinase receptors, acute models of metastasis, and MRI and PET scanning of bone damage during osteoporosis and arthritis. At the same time, imaging technologies are maturing and penetrating into more laboratories where they are helping to advance compounds to or toward candidate status. This session will highlight examples of how these techniques can drive drug discovery ranging from cellular HCS to whole animal studies both at the lead identification and lead optimization phases.
Structural Biology & Lead Optimization
Session Chairs:
Harren Jhoti, Astex Therapeutics Ltd., United Kingdom
Kendall Nettles, The Scripps Research Institute, USA
The use of structure-based drug design methods in the discovery of novel lead compounds has grown significantly in the last decade. This has been largely due to technology advances in structural biology that allow scientists to obtain protein/ligand structures in a timely manner to guide medicinal chemistry. As a consequence lead optimization programs are now able to more efficiently generate drug candidates with the desired properties. Furthermore, high-throughput methods in crystallography and NMR have also allowed structure-based methods to establish new approaches for lead generation, such as fragment-based discovery. This session will outline some of the key technology advances in structural biology and illustrate their application for structure-based lead generation and optimization.
ADME/Toxicology in Early Drug Discovery
Session Chairs:
Kirk McMillan, Exelixis, Inc., USA
Charles Crespi, BD Biosciences, USA
Early application of ADME/toxicology assays in support of lead validation/optimization has become a critical component of small molecule drug discovery in both pharma and biotech organizations. Implementation of in vitro assays for profiling metabolic stability, cytochrome P450 inhibition, cell (or membrane) permeability and physicochemical properties (solubility, lipophilicity, pKa, etc.), as well as assays for identifying hepatoxicity, reactive metabolites, HERG channel interaction and genotoxicity have become routine determinants of a candidate’s “drugability”. These profiling assays in conjunction with extensive in vivo DMPK/toxicology studies have resulted in the selection of better clinical candidates and reduced compound attrition. This session will address new technologies, current practices and future directions for this important aspect of preclinical drug discovery and development.
Knowledge Management & Extracting Value from Large Data Sets
Session Chair:
Robert Brown, SciTegic, USA
Access to accurate, comprehensive and up-to-date information is key to making good project decisions during the discovery process. This symposium will consider challenges and solutions in gathering, organizing, analyzing and presenting discovery information for a research organization, for both internal and externally generated data. The session will address new paradigms for information and knowledge management and the application of new techniques such as workflow to increase the efficiency and effectiveness of information organization and data analysis. We will also present the architecture, design and functionality of knowledge management systems and case studies of their operational effectiveness in the drug-discovery process. The impact of external resources such as target class knowledge bases in drug discovery and their integration into information and knowledge management systems will also be discussed.
Biomarkers for Pre-clinical & Clinical Evaluation of New Drugs
Session Chairs:
Nicholas Dracopoli, Bristol-Myers Squibb, USA
Thomas White, Celera Diagnostics, LLC, USA
Biomarkers are being increasingly used in all aspects of drug development from target discovery to life cycle management. Early implementation of biomarker discovery and assay development strategies into the clinical development plan is essential for clinical trial design and monitoring for first-in-class compounds, as well as for second generation compounds against the same target or pathways. The definition of biomarkers is very broad and encompasses genomic biomarkers (single nucleotide polymorphisms) used in genetic association studies to dynamic markers (quantitative gene expression assays by microarrays or qPCR, proteomics and the more traditional assay formats including immunochemistry and flow cytometry). Given the breadth of opportunities for the application of biomarkers in drug development from target identification to dose selection and prediction of drug efficacy and risk of adverse events, no single biomarker strategy exists for any therapeutic area, let alone an entire discovery and development portfolio. This symposium will focus on several successful applications of both genomic and dynamic biomarkers in drug development to illustrate possible strategies to reduce attrition and accelerate clinical development.
Drug Discovery for Diseases of the Developing World
Session Chairs:
Jose F. Garcia-Bustos, GlaxoSmithKline, Spain
Lisa Conte, Napopharma, USA
Pharmaceutical products and vaccines have revolutionized health care in industrialized countries during the last century. However, this progress has barely touched low-income countries where millions of people lack access to essential medicines that could potentially have a remarkable effect on the healthcare of a third of the world’s population. Closing the gap between potential and reality entails action in these areas: incentives for academic and industrial R&D in diseases endemic in low-income countries; financing and distribution in resource-constrained areas; drug affordability; effective drug regulation to avoid misuse and fake drugs; and multi-stakeholder community based education, training, and sustainability planning. The panel will explore (a) industry-based solutions to drug development, registration, and distribution in developing and emerging economies; (b) community health initiatives; (c) incentives for tropical disease R&D; and (d) non-profit initiatives to provide access to essential drugs.
Systems Biology & Confluence with Drug Discovery
Session Chairs:
John Aitchison, Institute for Systems Biology, USA
Ilya Shmulevich, Institute for Systems Biology, USA
Rapid technological advances in large-scale data collection coupled with model-driven mathematical and computational approaches are allowing scientists to gain a global and integrated view of physiology and pathophysiology. Unlike approaches that focus on individual molecules or small groups of interacting molecules, systems-scale approaches hold the promise of deciphering large dynamic molecular networks that dictate the phenotypic state and enable principled drug target identification, validation, and the development of targeted interventions. The systems approach to biology and medicine promises to transform the practice of medicine by changing it from a reactive discipline to a predictive, preventive and personalized discipline.
Posted under Equipment & Supplies, HT Screening, Medicinal Chemistry, Targeted Libraries, USA and Canada | Comments Off
HTG Introduces New ArrayPlate Testing Method; Gene Expression Technology Enables Researchers to Analyze Smaller Sample Sizes with Faster Results
Last Updated on Thursday, 4 May 2006 06:14 Written by admin Thursday, 4 May 2006 06:14
TUCSON, Ariz.–(BUSINESS WIRE)–May 2, 2006–HTG, Inc., a provider of novel array-based gene expression assay technology and services for the life sciences industry, today announced the availability of a new ArrayPlate to measure four genes in each well of a 384-well plate for high throughput screening and profiling. The ArrayPlate 384-4 enables researchers in the pharmaceutical and biotechnology industries to rapidly and accurately quantify RNA expression levels in cells treated with potential new drugs with high sample throughput, 10,000 or more samples per hour, and whole assay CV’s of less than 10%.
The new ArrayPlate 384-4 platform offering is based on HTG’s self-customized quantitative Nuclease Protection Assay (qNPA(TM)) technology, which allows researchers to test any sample type, including fixed tissue, using small sample sizes while avoiding the need for extraction, reverse transcription or amplification. The technology provides the absolute sensitivity to measure any gene desired, including low abundant genes. Instead of studying one gene at a time, researchers are also able to select a set of genes for simultaneous evaluation, a critical step in identifying the most promising drug compounds to treat complex, multi-factorial diseases.
Researchers can further utilize the 384-4 multiplexing capabilities by exploiting the power of gene signatures to reduce the whole cell assay false positive rate significantly, to as little as 0.05 percent, permitting discovery of weakly active compounds that would otherwise be missed. The platform provides highly sensitive and quantitative test results, including QSAR-quality dose response data and EC(50)’s, enabling clients to profile and optimize leads, compress drug discovery and development program timelines, increase program success and reduce costs.
The ArrayPlate 384-4 consists of a user-customizable plate with four elements of anchor oligonucleotides printed at the bottom of each well of the plate which allows researchers to measure up to four genes of their choice per well. This provides researchers with 1536 data points per plate. Combined with the ability to fully automate qNPA using off-the-shelf automation hardware, the ArrayPlate 384-4 technology permits the acquisition of 40,000 or more discrete gene measurements per hour.
“HTG’s ArrayPlate 384-4 technology enables high throughput screening at the level of gene expression, offering researchers a quick, easy and reliable method to economically and efficiently test more samples faster to address the issue the industry has faced with whole cell assay false positive rates,” said Bruce Seligmann, CSO, HTG. “Combined with qNPA QSAR capabilities, complete gene expression-based drug discovery programs can now be pursued from high throughput screening through in vitro and in vivo lead optimization. We are committed to developing and manufacturing highly sensitive and reproducible testing methods to help researchers wade through the growing amount of information available in the quest for new drug therapies.”
The ArrayPlate 384-4 is commercially available. For more information on the product, please call (520) 547-2827 or visit www.htgenomics.com.
About HTG
HTG provides ArrayPlate qNPA technology and services for the life sciences industry, addressing current unmet needs and enabling a new era of drug discovery and diagnostics. The company’s ArrayPlate technology platform enables the accurate, sensitive, reproducible and repeatable measurement of molecular signatures through the multiplexed measurement of RNA expression levels, DNA and protein levels and function. ArrayPlate qNPA data measure how drugs act and diseases are mediated at the level of whole cells, tissues, or organisms. This enables researchers to focus their resources by rapidly obtaining higher quality results than possible with other methods, in days rather than months, saving time and cost while addressing critical unmet needs. Privately held HTG is based in Tucson, Arizona. Investors in the company include Solstice Capital, Valley Ventures and Village Ventures. Additional information is available at www.htgenomics.com.
Posted under HT Screening, North America, Press Releases | Comments Off
Analysis of complex samples made easier
Last Updated on Thursday, 4 May 2006 06:11 Written by admin Thursday, 4 May 2006 06:11
A direct method for analysing complex samples, such as urine or milk, has been developed by researchers in the US.
Graham Cooks’ team at Purdue University conceived a sample introduction method for spectroscopic analysis that would avoid time consuming sample preparation.
Posted under Discoveries, Innovations and Patents, HT Screening, North America | Comments Off
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