Bio Screening Industry News

Munich and Freiburg, Germany, May 7, 2008 / b3c newswire / – CRELUX and ProQinase announced today that they have entered into a joint agreement to supply customers with crystal-grade protein kinases and readily available kinase complex structures.

Under the agreement, CRELUX and ProQinase will establish and continuously expand an off-the-shelf crystal-grade protein kinase portfolio, optimized and quality-controlled for successful crystallization. In addition, the two companies will work closely together to provide new crystal-grade protein or crystal structures, tailored to meet customers’ needs.

Recombinant protein kinases, optimized for crystallization, will be produced and exclusively marketed by ProQinase, while CRELUX will continue to provide customers with crystallization and x-ray crystallography services. CRELUX will support ProQinase by performing crystallization quality control for each crystal grade protein batch. At the same time, ProQinase will grant CRELUX privileged direct access to kinase crystal-grade protein.

“This new joint crystal-grade kinase platform offers tremendous advantages: It enables us to continue to focus on our core expertise – complex structure solution – while leveraging the expertise of ProQinase to significantly strengthen our capacities in protein expression,” commented Dr. Michael Schäffer, CEO of CRELUX.

“The combination of CRELUX’s expertise in protein crystallography and ProQinase’s know-how in kinase cloning and expression makes the two companies the partners of choice for all customers interested in kinase crystallography,” noted Dr. Christoph Schächtele, CEO of ProQinase.

CRELUX has used its state-of-the-art structural biology platform to solve more than 250 crystal and co-crystal structures for pharma and biotech companies. This platform encompasses all steps – from target cloning and expression all the way to high-throughput protein crystallization and in-house x-ray crystallography.

ProQinase, as part of its integrated protein kinase technology platform, offers more than 150 recombinant human protein kinases – all produced in-house – and provides all types of in vitro testing services, with more than 220 protein kinases.

Notes to editors

CRELUX GmbH ( www.crelux.com) provides fast and affordable access to co-crystal structures for biotech and pharma companies worldwide. Three dimensional structures of target-compound complexes are unique sources of information during the rational drug discovery process. Straightforward availability of structural data at an early stage of the drug development process significantly enhances productivity and success rates during hit selection, lead generation, and lead optimization. CRELUX has streamlined the processes of structure generation and solved hundreds of co-crystal structures using an integrated technology platform. In addition to customer designed projects crystallization conditions of numerous relevant therapeutic targets are available within the Off-The-Shelf Program of CRELUX. Off-The-Shelf target structures are delivered at a fixed price and short turn around times, facilitating affordable access to structural information.

ProQinase GmbH ( www.proqinase.com) provides an Integrated Protein Kinase Technology (iProKiTe®) Platform for preclinical drug development of protein kinase inhibitors. More than 150 highly active recombinant kinases are offered for sale and more than 220 kinases are available for in vitro testing services (HTS and selectivity profiling etc.). Cellular and in vivo test systems including orthotopic tumor models allow further testing of lead compounds. A Clinical biomarker analysis service supports the evaluation of clinical trials.

Heidelberg, Germany, November 29, 2007 /b3c newswire/ — Graffinity Pharmaceuticals GmbH announced today that it has entered into its second drug discovery collaboration with Pfizer, Inc. Through the collaboration, Graffinity will provide Pfizer with access to its proprietary, fragment-based screening technology for use in screening Pfizer drug targets. The agreement is Graffinity’s sixth discovery collaboration since it was established as an independent company in 2006.

Kristina Schmidt, CEO of Graffinity, stated, ”Graffinity was established almost two years ago as an independent company to commercialize its proprietary fragment-based discovery technology. To have entered into six collaborations in such a short period of time highlights the outstanding progress we have made, underscores the potential both of our technology and business model, and positions us as a leader in this growing area of drug discovery.”

About Graffinity Pharmaceuticals GmbH - www.graffinity.com

Heidelberg, Germany based Graffinity Pharmaceuticals is a leader in the field of small molecule fragment based drug discovery. The company pursues high-profile drug discovery collaborations with leading pharmaceutical and biotechnology companies worldwide. Graffinity employs a flexible business model which allows it to tailor programs to the specific needs of each partner and offers numerous benefits to its customers on a straightforward fee-for-service basis. Graffinity’s fragment screening platform combines chemical microarrays with a proprietary method for the standardized, label-free detection of compound-protein interactions via SPR imaging. The company’s rapid and scalable drug discovery technology explores a rich chemical universe to identify drug fragments which address challenging drug targets. With its 110,000-compound library that contains 23,000 true fragments, Graffinity possesses one of the most diverse fragment libraries. Graffinity has established collaborations with pharmaceutical and biotechnology partners including Amgen, Boehringer-Ingelheim, Genentech, Pfizer and Merck-Serono.

Graffinity’s unique fragment based discovery platform has been invented in 1998, and has been in routine industrial use since 2002 in screening more than 60 drug targets.

Innovating kinase inhibitor development is the key to successful clinical development. At Informa Life Sciences 7th Annual Protein Kinases Congress hear the latest thinking and strategies towards creating a selective inhibitor. Learn about new targets, industry trends in structure-based drug design, clinical case-studies and discuss the issue of cardiotoxicity.

For more information visit: http://www.iir-events.com/IIR-Conf/page.aspx?id=9547

OTAVA, the company that specializes in combinatorial chemistry, fluorescent probes and drug discovery technologies, offers unique ProHit compounds displaying inhibitory activity against distinct protein kinases.
ProHit Compound Sets are distributed on an exclusive basis and can be used in the development of drugs targeting protein kinase enzymes.

Every Kinase ProHit Compound Set is organized as a cluster of similar compounds having the following features:

1. obtained by organic synthesis
2. showed high inhibitory activity towards the targe (IC50 less than 1 uM for the most active compounds)
3. have good drug-likeness
4. showed chemical stability
5. showed chemical feasibility
6. free of Intellectual property
7. checked in specialized databases to define patentability

Protein Kinase CK2 ProHit Set (CK2ProHit) is now available.
For more information, please contact us

http://www.otavachemicals.com

More Kinase ProHit Sets are on the way!

New Hope, PA — (SBWIRE) — 10/10/2007 — Bucks County’s Institute for Hepatitis and Virus Research (IHVR) and BioLeap have entered into a collaboration to develop new therapeutic compounds for the treatment of Hepatitis C. Up to 50% of patients treated with current standard therapies do not respond adequately and often suffer serious side effects from the drugs. Thus there is a critical need for new tools to treat this disease. By combining BioLeap’s leading edge computational fragment-based design capabilities with the IHVR’s extensive experience and in-depth knowledge of viral diseases, the collaboration will result in new classes of lead drug molecules with novel modes-of-action.

Of particular interest to the IHVR is BioLeap’s proprietary technology that rapidly calculates the free energies, or affinities of interactions between small molecular fragments of potential drugs and biomolecular structures of the proteins they will target, displaying the distribution and orientation of these fragments. This information provides a unique insight into how small molecules bind into key protein binding sites that cannot be achieved from the static crystal structure alone, or from methods that can only measure the enthalpic properties of binding. In addition to lead discovery, the quantitative free-energy based analysis of protein-drug-fragment interactions adds significant value to the lead optimization process. In combination, this proprietary approach provides chemists and biologists the information they need to assemble, fragment by fragment, a completely new molecule that not only optimally binds to the targeted protein site but also has properties desirable in a drug, including solubility and bioavailability.

Commenting on the collaboration, BioLeap’s Gerry Evans, Executive Vice President of BioLeap, noted: “Dr. Tim Block and his team at the IHVR are renowned for their work in this field. We are very excited by the opportunity to focus our combined expertise on this important target.”

Dr. Tim Block, president of the IHVR, is enthusiastic about the prospects for this collaboration. “One approach in discovering new treatments is the time and labor intensive process of screening tens or hundreds of thousands of molecules from compound libraries. BioLeap’s technology provides a potential shortcut by eliminating the need to screen compound libraries, while significantly broadening the field of chemical diversity. The molecules designed by BioLeap are not limited by what is present in any compound library. This greatly increases our odds of finding a potential drug that precisely targets the hepatitis C virus and that will not easily succumb to viral resistance. Once BioLeap has identified several candidate molecules, our scientists will test their effectiveness on the hepatitis C virus. Based on these results, we will repeat this iterative process until we have found the ideal drug.”

About the Institute for Hepatitis and Virus Research:
Established as the research arm of the Hepatitis B Foundation, the mission of the Institute for Hepatitis and Virus Research is to use discovery science to find new therapies for viral hepatitis and liver cancer; to advance its research discoveries through traditional scholarship and educational opportunities; to nurture biotechnology through technology transfer and new company formation; and to promote public health outreach programs to improve the quality of life for those with viral hepatitis.

About BioLeap:
Bioleap is a leader in computational fragment-based drug design. The company’s proprietary design technology and process successfully addresses one of the biggest problems in preclinical drug discovery: limited chemical diversity of compound libraries. Development collaborations span a broad spectrum of target proteins including: kinases, nuclear hormone receptors, metalloenzymes, and metalloproteases.

(PRLog.Org) – Oct 17, 2007 – MONROVIA, CA – Dr. Stephen K. Burley, Chief Scientific Officer and Senior Vice-President Research at SGX Pharmaceuticals, Inc. located in San Diego, CA will give the Keynote presentation at GTCbio’s Drug Design & Lead Discovery conference – one of six tracks at the 3rd Modern Drug Discovery & Development Summit on November 28-30, 2007 at the Hyatt Regency San Francisco Airport.

Dr. Burley’s presentation will cover fragment-based discovery of selective, orally bioavailable tyrosine kinase inhibitors for targeted treatment of human cancers with examples from SGX’s FAST™ (Fragments of Active Structures) platform.

The fragment-based drug discovery platform utilizes high-throughput X-ray crystallography for lead identification/optimization. The process exploits crystallographic screening to detect, visualize and identify small ligands (MW 150-200) that are bound to the target protein. Each member of the FAST™ fragment/scaffold library was selected to be amenable to rapid chemical elaboration at two or three points of chemical diversity using parallel organic synthesis. Initial lead optimization involves using SGX’s knowledge of the co-crystal structure of the target-fragment complex and advanced computational chemistry tools to guide synthesis of small focused linear (one-dimensional) libraries. These linearly elaborated fragments/scaffolds are then evaluated with in vitro biochemical and cellular assays and co-crystal structure determinations. Thereafter, optimal variations at each point of chemical diversity are combined to synthesize focused combinatorial (two- or three-dimensional) libraries that are again examined with assays and crystallography. (The potential chemical diversity of the fully elaborated FAST™ fragment/scaffold library far exceeds 160 million compounds.) Active compound series are prioritized for further medicinal chemistry and compound development efforts using the results of in vitro and in vivo ADME and in vitro toxicology studies. Successful applications of the FAST™ fragment-based lead discovery/optimization process will be presented for a portfolio of well validated oncology targets.

The 3rd Modern Drug Discovery & Development Summit features over 150 speakers participating in 6 concurrent conferences, 6 study sessions and 3 pre-conference workshops. Tracks include Biological Therapeutics, Drug Delivery Technology, Translational Medicine, Drug Design and Lead Optimization, Emerging Targets, and Pharmaco – Kinetics, Dynamics, Genomics and Genetics. For more information, visit www.gtcbio.com.

HOPKINTON, Mass., Aug. 7 /PRNewswire-FirstCall/ — Caliper Life Sciences, Inc. today launched the Caliper LabChip(R) EZ Reader(TM) Series, delivering a complete range of products for in-house kinase profiling. The series, which complements the existing LabChip 3000 system, Caliper’s most sophisticated system for drug discovery, includes the new EZ Reader II system, a bench-top reader to use for real-time kinetic analysis with push-button operation, and the EZ Reader system, formerly the DeskTop Profiler(TM) system. Each product in the EZ Reader Series utilizes Caliper’s LabChip microfluidic-based screening technology to yield high-quality, reproducible data to help pharmaceutical researchers more confidently qualify potential lead candidates.

The EZ Reader Series features innovative systems that rapidly profile compounds against a diverse kinase panel in a timely and cost-effective manner. The Series complements Caliper’s existing offerings for kinase profiling. The EZ Reader system features a four-sipper Caliper LabChip microfluidic device, while the EZ Reader II system provides a choice of either a 4-sipper or a 12-sipper LabChip device to run assays with up to three times higher throughput. The EZ Reader II system also enables real time kinetic analysis, allowing researchers to study enzyme behavior over time in mechanism-of-action (MOA) studies. Its compact, bench-top size and push-button operation delivers a high level of functionality without a large footprint or the need for highly skilled operators. Caliper’s ProfilerPro(TM) kinase reagent profiling kit, which allows broad range, rapid kinase profiling in-house, accompanies each system.

“The EZ Reader II system extends the benefits of Caliper’s LabChip technology to academic laboratories, small biotech companies and distributed therapeutic groups,” said Rick Bunch, Business Unit Manager, LabChip Systems, Caliper Life Sciences. “Its inclusion in the EZ Reader series demonstrates Caliper’s commitment to delivering technology and services that fulfill a broad range of customer needs.”

The EZ Reader II system is currently on display at the Drug Discovery & Development of Innovative Therapeutics (DDT) conference in Boston. For additional information, please visit Caliper Life Sciences at booth 628.

About Caliper Life Sciences

Caliper Life Sciences is a leading provider of cutting-edge technologies enabling researchers in the life sciences to create life-saving and enhancing medicines and diagnostic tests more quickly and efficiently. Caliper is aggressively innovating new technology to bridge the gap between in vitro assays and in vivo results and then translate those results into cures for human disease. Caliper’s portfolio of offerings includes state-of-the-art microfluidics, lab automation & liquid handling, optical imaging technologies, and discovery & development outsourcing solutions. For more information please visit http://www.caliperLS.com.

Caliper, LabChip, DeskTop Profiler, ProfilerPro and EZ Reader are trademarks of Caliper Life Sciences, Inc.

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. 

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

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

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.