Archive for the ‘Compound Libraries’ Category
Molecular Target for Screening: G-Protein-Coupled Receptors
Last Updated on Friday, 20 August 2010 06:48 Written by Editor Thursday, 19 August 2010 03:10
Newark, DE. August, 2010 – Press Release – TimTec, LLC. – Molecular Target for Screening: G-Protein-Coupled Receptors, ActiTarg-G
G-Protein-Coupled Receptors are the largest gene families in the human genome and, rightfully so, have become the leading molecular target in 2008. In 2009 SBS April meeting in Lille, France, followed-up with screening trends report stating that “GPCRs are expected to replace protein kinases as the most common molecular target used by HTS laboratories.”
GPCRs are the largest family of cell surface receptors being integral to the number of cellular and physiological functions, including light sensing, smell, appetite control, insulin secretion, and blood pressure modulation. These receptors generally have a seven-membrane spanning alpha-helical topography, and while these receptors are similar in overall structure and function, they differ in key amino acid residues. The potential for this super family of receptors to reveal small molecule modulators of a significant biological function has been responsible for the focus of intense drug discovery efforts.
TimTec GPCR Ligands library is called ActiTarg-G. It currently counts 2,300 molecules available in various formatting options, and can be delivered in vials or in 96 or 384-well plates. ActiTarg-G is the set of diverse molecules that contain chemical lattices present in compounds reported in the technical or patent literature to possess GPCR-ligand properties.
Contact Information to schedule free consultation:
TimTec LLC
Harmony Business Park A-301
Newark DE 19711
Tel 302 292 8500
Fax 302 292 8520
Web: http://www.timtec.net/news/timtec-news/actitarg-g-gpcr-ligandshtml.html
About TimTec
TimTec LLC is a privately held company located in Newark Delaware, USA. It was founded in 1995 and began its work in the areas of acquisition and distribution of synthetic organic and natural compounds and collections, custom synthesis, and laboratory equipment to become a full service partner for drug discovery. TimTec has established a global network of thousands of scientists from research centers around the world. International customers include major pharmaceutical, biotech, agricultural, and educational companies and institutions, which use TimTec products for research and development programs.
Evotec Gains Access to Hypha’s MycoDiverse Natural Products Library
Last Updated on Thursday, 13 May 2010 12:43 Written by Editor Thursday, 13 May 2010 12:43
Evotec negotiated access to U.K.-based Hypha Discovery’s MycoDiverse™ fungi-derived natural product screening library. The deal means Evotec will be able to offer the library to clients through its hit and lead identification services.
Hypha currently has access to over 2,500 strains of higher basidiomycete and ascomycete fungi, many from South American and South East Asian rainforests. The firm’s MycoDiverse library comprises low-molecular weight compounds derived from temperate and tropical basidiomycete fungi (mushrooms and toadstools).
The library is generated using a proprietary fermentation technology that uses stimulators and growth media to reproduce stress of life for rainforest fungi. Hypha claims this promotes the production of biologically active molecules with unusually high chemical novelty.
“We see access to Hypha’s high-quality natural product collection as a logical step towards offering our customers further choices for lead identification,†comments Mark Ashton, Ph.D., Evotec’s evp business development.
Posted under Collaborations, Compound Libraries, Press Releases | No Comments
Product Focus: Automated Liquid Handling
Last Updated on Thursday, 6 May 2010 10:13 Written by Editor Thursday, 6 May 2010 10:13
Liquid handlers are sold in a variety of fluid-dispensing configurations, from single-channel through eight (one row of a 96-well microtiter plate), 96, and 384 channels. As the successors to manual pipettes, automated liquid handlers are the principal enablers of rapid experiments and assays conducted in tubes, vials, or microtiter plates. Liquid handlers are often just one component of systems consisting of microplate handlers, washers, readers, stackers, shakers, and incubators. Automation became necessary as assays were miniaturized from vials to tubes, and finally to microplates, and as researchers switched from radionuclide-based assays to tests that used non-radioactive detection.
Biology, medical testing, and screening of development-stage drugs are the primary markets for automated liquid handling. The energy, environmental, and heavy industries also use liquid handlers when accuracy and reproducibility, but not necessarily high throughput, are desired. “Any time you work with many samples and small quantities of fluids, automating liquid handling with a workstation will provide good return on investment,†says Scott Eaton, director of robotics marketing at Hamilton (Reno, NV).
Assessing workflow requirements is essential when selecting an automation system. Liquid transfers take time, which adds up rapidly as dispensing and other operations increase. Users who work with labile or highly toxic samples or reagents may prefer to process a smaller number of plates per run in order to move them rapidly through the protocol.
Another factor to consider, Eaton says, is the effect of physical forces on very small liquid-dispensing volumes used in higherdensity plates. “While 96-well plates remain the most common, 384- and even 1,586- well systems that employ sub-microliter volumes are gaining in popularity. At these volumes, evaporation and absorption onto the plastic plate surface become issues.â€
Automated liquid handlers have evolved from automated pipetting systems to workstations that employ liquid handling as one component, according to Nance Hall, vice president for automation and detection systems at PerkinElmer (Waltham, MA). Today’s systems perform washing, incubation, and plate manipulation in addition to dispensing. “In the past, liquid handlers performed just one function; today, they are ‘application solutions’ in which liquid handling is part of a larger picture,†Hall says.
Differentiators
Eaton believes a combination of ease-ofuse and flexibility in software is an important differentiator when selecting an automated liquid handler. “Some software is very easy to use, but it’s locked into specific applications.†The best of both worlds, he says, is a software package that presents operations graphically, provides “wizards†or templates for routine tasks, and that adapts to different assays. 
Hall suggests that potential buyers analyze their liquid-handling needs the way a cook examines a recipe. “What are the ‘ingredients’? What labware are we dispensing from and into? What do I expect from the automation component? What volumes are involved, and what sample-tip options are available?†Hall says. “Users who fail to optimize the liquid handler’s fluidics design to desired volumes will be forced to compromise either on performance or throughput.â€
Users should weigh throughput considerations when considering a liquid-handler purchase, says Jason Greene, liquid-handling product manager at BioTek (Winooski, VT). “The cutoff point for automation versus a multi-channel handheld pipette is several strips [rows or columns on a microplate] per day,†Greene says.
This seems like a small number of assays to justify the investment in automation, but as Greene notes, liquid handling is just one component of what may be a complex workflow. “Operating manually, users must work through the various reagent additions, incubations, washing, and reading steps,†he says. “Nobody likes to wash microplates. It’s pretty easy to get users to buy into the idea of automation on that function alone.†Moreover, he says, even low-throughput labs come to value the reproducibility of automated systems.
For Nadine Gassner, associate director of the Chemical Screening Center at the University of California-Santa Cruz, experience with a particular vendor is a major factor in selecting a liquid-handling system. The center, which performs highthroughput screening on natural-product and newly synthesized drug candidates, has the capability of testing hundreds of thousands of compounds in one experiment using 96- and 384-well plates.
Gassner had already been using a PerkinElmer plate reader. During the startup phase of the screening center, she visited the company and was impressed with the ability of its liquid handlers to service a variety of assays. “We were also looking for a strong industry track record and considered our experiences with PerkinElmer’s excellent service.â€
Angelo DePalma holds a Ph.D. in organic chemistry and has worked in the pharmaceutical industry. You can reach him at angelo@adepalma.com.
Posted under Compound Libraries, Compound Screening, Press Releases | No Comments
Developments in Focused Kinase Libraries
Last Updated on Monday, 11 January 2010 03:14 Written by Editor Monday, 11 January 2010 03:14
Chemical libraries have long been a mainstay in the search for new pharmaceutical compounds, and they have been created using many different paradigms. Vast diverse collections of unique compounds have been screened at high throughput to find appropriate effects on target proteins. Such large libraries continue to be used for drug discovery, but screening smaller, more focused libraries, can provide more efficient solutions with better overall hit rates.
Ten years ago, BioFocus®, a Galapagos company, launched a nonexclusive compound library specifically designed to target serine-threonine and tyrosine kinases. This library, SoftFocus® Kinase library one (SFK01), was designed to mimic the binding of ATP to the catalytic (hinge) region and had a rather simplistic design based around an aminopyrimidine core (Figure 1).
Targeting Kinases
| Protein kinases are enzymes that phosphorylate substrate proteins at specified residues such as serine, threonine, and tyrosine. The phosphorylation of the substrate protein initiates a cascade, that in turn, modulates the transcription of a gene or set of genes. Kinases play pivotal roles in modulating diverse cellular activities, including growth, differentiation, metabolism, adhesion, motility, and death, and have been implicated as important mediators of certain forms of cancer.
Kinases, therefore, represent key druggable target proteins. The initial realization that most kinases possess highly conserved catalytic domains initially made kinase targets ideally suited for compound screening via focused chemical libraries in which the library compounds were specifically created to bind to the catalytic (hinge) regions. Despite the slightly higher costs generally associated with the design and synthesis of such focused libraries compared to large and diverse compound collections, true savings can be gained as a result of shortened project cycles coupled with the reduced costs of screening, storage, and quality control of a smaller screening library. The increasing wealth of structural data available along with a number of new techniques such as in silico design has enabled the continual development of kinase-focused collections, providing increasingly more sophisticated chemical structures. One of the key benefits of this is that the current range of SoftFocus kinase libraries has been designed to target additional binding modes to those involving the hinge region; most notably the DFG-out binding mode and the novel binding mode first observed in the kinase PIM-1. |
In Silico Design
Current in silico design processes enable automated docking and scoring of scaffold ideas into a variety of known x-ray structures that have been selected, not only for broad coverage of the kinome, but also different conformational states of individual kinase enzymes. The design premise is that, if the core of the molecule or scaffold contains the key recognition groups for binding into one of the known conformational states, it has the potential to target any kinase.
However, as different side chains or monomers are added, the potential to gain specificity for one target over another becomes reality. The various docking methods used in the design of the BioFocus libraries include hinge binding, the DFG-out model, and novel binding modes.
Hinge Binding
| Hinge-binding library designs are validated by docking a minimally substituted scaffold into various different high-resolution kinase x-ray structures. These structures have been selected from across the phylogenetic tree to ensure broad coverage of tyrosine and serine/threonine kinases.
The BioFocus Kinase Toolkitâ„¢ provides a two-dimensional map (2D Roadmap) of the key ligand-binding features within a customized ATP-site model, allowing predictions of affinity, selectivity, and likely off-target issues based on the compositions of the individual sub-sites. This knowledge can then be used to select the appropriate side chains or monomers with which to decorate the scaffolds. |
DFG-Out Model
An approach to the design of kinase libraries with higher selectivity potential is to target the DFG-out allosteric pocket adjacent to the ATP site. BioFocus has developed a generalized binding model of the DFG-out pocket that enables the targeting of a range of inactive kinase conformations.
Binding Modes
”><img width=){kind=link}
Focusing on Success
By constantly refining the compounds using in silico methods, including those described above and with the development of innovative in silico models and applications such as Cresset BioMolecular’s molecular Field technology, the latest advances in kinase research can be incorporated into novel libraries. Consequently, this may also provide a strong intellectual property position to those who screen them. Indeed, based on the screening of SoftFocus kinase libraries alone, over 70 known patents have been applied for or granted.
A recent example from Galapagos highlights this. Following a screen of some 16,000 BioFocus focused kinase compounds, three hit series were identified that showed structure-activity relationships against a novel rheumatoid arthritis target. Two of these compound series were progressed to the hit-to-lead phase and subsequently one series was optimized, and a compound is currently undergoing clinical trials. The project time from screening to preclinical candidate nomination was three years.
There is no doubt that the drug discovery process should be shortened whenever possible. It is essential to improve the lead discovery process. Focused compound libraries such as the SoftFocus collection have the inherent capabilities to provide a robust hit discovery process, with good hit-to-lead conversion rates and shorter development times.
Furthermore, such libraries can maximize the benefit of new techniques such as in silico modeling, enabling them to be consistently developed over time. BioFocus has also maintained flexibility in its library-generation processes using these techniques, which has enabled the development of novel libraries with proven results.
Source: genengnews.com
Posted under Compound Libraries, Compound Screening, Press Releases | No Comments
Computational Method Points To New Uses, Unexpected Side Effects Of Already Existing Drugs
Last Updated on Tuesday, 15 December 2009 04:19 Written by Editor Tuesday, 15 December 2009 04:19
Scientists at the University of North Carolina at Chapel Hill School of Medicine and the University of California, San Francisco have developed and experimentally tested a technique to predict new target diseases for existing drugs.
The researchers developed a computational method that compares how similar the structures of all known drugs are to the naturally occurring binding partners — known as ligands — of disease targets within the cell. In a study published this week in Nature, the scientists showed that the method predicts potential new uses as well as unexpected side effects of approved drugs.”This approach uncovered interactions between drugs and targets that we never could have predicted simply by looking at the chemical structures,” said senior study author Bryan Roth, M.D., Ph.D., professor of pharmacology and director of the National Institute of Mental Health Psychoactive Drug Screening Program at UNC. “We may now have a way to predict what side effects are likely to occur from treatment before we even put a drug into clinical testing.” Roth is also a member of the UNC Lineberger Comprehensive Cancer Center.
Many of the most successful drugs on the market today are being prescribed for ailments that are quite different from the ones they were originally designed to treat. Viagra, for instance, was once intended for coronary heart disease but now is used to combat erectile dysfunction. The discovery of surprising uses of developed drugs can sometimes be the result of serendipity, as unforeseen side effects emerge from clinical trials. In the past, researchers have tried to predict drug interactions by looking for chemical similarities among the possible targets of pharmaceutical compounds.
However, some drug targets which look very similar to one another bind very different ligands, and some targets that don’t have any obvious similarity bind similar ligands, says Brian Shoichet, Ph.D., co-senior study author and professor of pharmaceutical chemistry at the University of California at San Francisco. “So if instead we were to organize targets by the ligands they recognize, it could reveal different patterns than traditional approaches, and illuminate new opportunities for drugs to bind to unexpected targets.”
A team of researchers led by Roth and Shoichet did just that, comparing the structures of 3,365 FDA-approved and investigational drugs against the structures of hundreds of targets, defining each target by its ligands. They then honed in on thirty of the strongest predictions, validating the actual physical interactions between the drugs and targets in wet laboratory experiments.
In one of their follow-up experiments, the scientists investigated the molecular targets of the hallucinogenic substance dimethyltrytamine (DMT), which had previously been postulated to act through a site known as the sigma-1 receptor. Using the computational approach, Roth and colleagues found that DMT had a high affinity for serotonin receptors, including the binding site for LSD, another hallucinogen.
They also showed that the substance is hallucinogenic in normal mouse models but not in ones lacking the serotonin receptor. Roth says the power of their approach is it can be used to uncover the real targets of pharmaceutical compounds quickly and efficiently, and will probably lead to a greater understanding of the many molecular targets of each drug.
“Drugs are not as selective as we once thought,” said Roth, who is also a professor in the School of Pharmacy’s medicinal chemistry and natural products division. “It turns out that the most non-selective drugs are frequently the most effective for complex diseases. Rather than ‘magic bullets,’ we need to come up with ‘magic shotguns’ that hit more than one molecular target at a time. We could use this computational approach to identify the drugs that hit the right targets and miss the wrong ones.”
Study co-authors from UNC include Vincent Setola, research associate professor; Atheir Abbas, former graduate student; Sandra J. Hufeisen, senior research assistant; Niels H. Jensen, research associate; Michael B. Kuijer, research technician; Roberto C. Matos, research technician; Thuy B. Tran, research technician; Ryan Whaley, research technician; and Richard A. Glennon. The paper’s first author is Dr. Michael Keiser, from the UCSF side of the collaboration. Also from UCSF were Drs. John Irwin, Christian Laggner and Jerome Hert, and PharmDs Kelan Thomas and Douglas Edwards.
Funding for the studies at UNC and at UCSF came from the National Institutes of Health.
ScienceDaily (Nov. 7, 2009)
Posted under Compound Libraries, Compound Screening, Drug Development, Press Releases | No Comments
Trophos launches the new generation of its fast plate imaging instrument, the Plate RUNNER HD
Last Updated on Thursday, 22 October 2009 11:09 Written by Editor Monday, 12 October 2009 03:31
Marseille, FRANCE, 2009 September 29 – Trophos SA, a clinical stage pharmaceutical company developing innovative therapeutics for indications with under-served needs in neurology and cardiology, announced today the launch of the new generation of its fluorescence fast plate imaging system, the Plate RUNNER HD(R).
Trophos originally developed the Plate RUNNER HD(R) to speed up its own screening campaigns for drug discovery and development. The company has now implemented an improved version which offers much better resolution and allows imaging of the 7mm well of the standard 96 plate in matrices of up to 8192 x 8192 pixels. This positions it as the superior alternative to the traditional automated microscope in a wider area of cellular and small organism imaging applications such as neurite outgrowth or C.elegans screens. The Plate RUNNER HD(R) is protected by patents granted in the USA and Europe.
“The Plate RUNNER HD(R) has now reached both a performance and an operational level that allows it to be widely used in various imaging platforms,” said Damian Marron, CEO of Trophos. “We have optimized it by regular use in our screening and research platforms. Use in other labs such as the Neuronal Cell Biology & Pathology research unit directed by Dr Christian Neri at the Inserm Psychiatry and Neurosciences Centre (Paris, France) and the Laboratory of Motor Neuron Biology directed by Dr Alvaro G. Estévez at the Burke Medical Research Institute (NY, USA) has confirmed its performance.” (For further information, see http://www.broca.inserm.fr and http://www.burke.org).
The Plate RUNNER HD(R) fills the gaps between the low sensitivity/low resolution/cell consuming fluorescence plate readers, the high sensitivity but non-imaging flow cytometer, and the slow, poorly automated and small field fluorescence microscope. It does this by allowing whole well/full plate imaging in just 2 minutes 40 seconds for 96 images of 1024 x 1024 pixels, 8 minutes at 4096 x 4096 resolution and 25 minutes at the extremely powerful 8192 x 8192 resolution. The maximum resolution gives details as fine as 1 micron, which covers the vast majority of cellular imaging applications.
“The instrument is not only the source of our pipeline – nearly 1 million compounds screened in eight years – but also an everyday research tool that does in two minutes a job that usually requires a week manually,” said Pierre Delaage, Head of Development of Trophos Instruments. “Using exclusively open data formats, the Plate RUNNER HD(R) integrates smartly and smoothly with all existing imaging and data processing environments with no hidden extra costs. It is also a “green product” using at least ten times less electrical power for illumination than its competitors. It has the important advantage of having a lower price and TCO than the traditional microscope-based instruments.”
Dr Christian Neri, Research Director at the Psychiatry and Neuroscience Center of Inserm in Paris, stated “We have been using the Trophos screening system since its first commercial version; it allowed us to simply and rapidly automate our screening protocols on C.elegans worms and on cells. To move further in C.elegans screens we needed a far higher resolution without sacrificing light, sensitivity and field. We have now seen that Trophos’ latest instrument meets perfectly our very stringent requirements.”
“We continue to directly sell and support the Plate RUNNER HD(R) and are now looking to set up a commercial and industrial partnership to address more widely the global market opportunity,” added Marron. “The Plate RUNNER HD(R) offers unique performance and can be a great fit for imaging solutions manufacturers and vendors, to exploit opportunities for example in the area of small organism or angiogenesis screens as well as cellular screens.”
About the Plate RUNNER HD(R): Developed by Trophos since 1999 initially for its own HTS platform, The Plate RUNNER HD(R) is a rapid fluorescence 96-plate imager giving full 7mm well images in single snapshots (ie no mosaic reconstruction), embedding three commonly used wavelength illumination lamps using fast-switching LED technology, thus leading to more homogeneous light, very long life time (100 000 hours against 5000 hours for xenon or mercury lamps), higher speed and dramatically reduced maintenance costs. Images are given in standard 1024 x 1024 definition but also in higher 2048 x 2048, 4096 x 4096 and even 8192 x 8192 pixels definition, leading to details of about 1 micron in size.
Compared to classic automated microscopes, The Plate RUNNER HD(R) is much more simple, integrated, automated, robust and fast; it has no oculars (eyepieces), no huge frame, no complicated auto focus system, no complicated settings, no complicated software, and does not need any cooling/heating delay between illumination sessions nor painful recalibration between sessions. Built on modular, open and interoperable design and data formats, it is compatible with any existing image processing platform. Training for common tasks is achieved in less than 1 hour, and there is no need of high skilled people to install or set it up.
Driven by Trophos proprietary software running on standard low cost PCs and using advanced real time programming techniques coming from the industry, the device reliably acquires 96 images at 1024 x 1024 definition in just 2 minutes 40 seconds (for a standard 488nm excitation and 200ms exposure time), 8mn for 4096 x 4096 images and 25mn for 8192 x 8192 images.
The device is patent protected in France, Europe and USA. Patent is pending in Canada and Japan. Detailed specifications are available here (http://www.trophos.com/download/pr_datasheet.pdf).
About Trophos: http://www.trophos.com Trophos is a clinical stage pharmaceutical company developing innovative therapeutics from discovery to clinical validation for indications with under-served needs in neurology and cardiology. The Company has a novel and proprietary cholesterol-oxime based chemistry platform generating a pipeline of drug candidates, with the lead product, olesoxime (TRO19622), in phase II clinical trials and a second product, TRO40303, planned to enter the clinic in 2010. Trophos’ mitochondrial pore modulator compounds enhance the function and survival of stressed cells via modulation of dysfunctional mitochondria through interactions at the permeability transition pore (mPTP). Recently published clinical studies support the therapeutic rationale for mitochondria targeted drugs in neurology (Alzheimer’s disease) and cardiology (ischemia-reperfusion injury), which Trophos is uniquely placed to exploit.
Trophos has not only invested in science but also in technology such as the Plate RUNNER HD(R), which is a key reason why Trophos was able to bring products into phase II clinical trial after only 8 years, instead of the 12-15 or even 20 years commonly observed”.
For further information, please contact:
Andrew Lloyd & Associates Andrew Lloyd / Neil Hunter Tel: +44 1273 675100 allo@ala.com
Source: medadnews.com
Posted under Compound Libraries, Compound Screening, Industry News, Press Releases | No Comments
Zelinsky Institute Inc. announced collaboration with ART-CHEM
Last Updated on Saturday, 10 October 2009 06:10 Written by admin Saturday, 10 October 2009 06:10
Zelinsky Institute Inc. (Newark, DE, August 2009) – Zelinsky Institute Inc. expands its partnership and supplier network with the announcement of collaboration with one of the premier fine chemistry companies – ART-CHEM, which originated from Moscow, Russia, and has started its operations in Berlin, Germany, in 2005. ART-CHEM specializes in synthesis of highly diverse and rich in unique scaffolds HTS compounds and building blocks. The entire line of ART-CHEM product offerings is going to be available via Zelinsky Institute Inc., which is headquartered in and currently operates from Delaware, USA, offices.
ART-CHEM founder, Dr. B. Ugrak, comments, “We are pleased to become a part of Zelinsky Institute, a recognized supplier of specialty chemicals. Together we can provide greater value serving our, now, joined customer base.†Zelinsky Institute CEO, Dr. M. Niazoff, agrees adding, “We are happy to have ART-CHEM high quality fine chemistry products and service capabilities accessible via Zelinsky Institute. Together, we are looking forward to growing our market fueled by ever-evolving research demands.â€
Collaboration aims at making ART-CHEM products and services known and easily accessible for existing and prospective Zelinsky Institute Inc. customers worldwide. September 2009 product databases distributed by Zelinsky Institute Inc. are going to include ART-CHEM’s drug-like and chemically diverse compounds for screening, building blocks, and intermediates. Zelinsky Institute Inc. is going to coordinate procurement, orders, and consolidated delivery of HTS products. Zelinsky Institute Inc. and ART-CHEM collaboration is open to custom projects going beyond the supply of just existing fine organic chemistry. For recently launched databases, products and services, inquiries, orders, and customized solutions please contact \n info@zelinsky.com .
Zelinsky Institute Inc., located in Delaware, USA, is the official representative of Zelinsky Institute of Organic Chemistry of the Russian Academy of Sciences (ZIOC) in Moscow, Russia. ZIOC is one of the world’s largest scientific centers in the fields of organic chemistry, organic catalysis, and chemistry of biologically active compounds. The Institute was founded on February 23, 1934, following the Decision of the Presidium of the Academy of Sciences of the USSR.
Zelinsky Institute Inc. began its operations in the USA in 1993 to establish the first commercialization bridge in compound supply industry linking Former USSR research centers unique chemistries and R&D service capabilities with Western life-science industries demands. Among Zelinsky Institute Inc. first customers were DuPont, Merck, Johnson&Johnson, and Ely Lilly. Â Zelinsky Institute Inc. has expanded its markets and partnerships and welcomes new global customers and scientific challenges.
Contacts:
ART-CHEM GmbH
Campus Berlin-Buch, Haus B55
Robert-Roessle-Strasse 10
13125 Berlin, Germany
Phone: +49 (0)30 9489-2180
Fax:Â Â Â Â Â +49 (0)30 9489-2181
Zelinsky Institute Inc.
POB 8941, Newark, DE, 19714 USA
For products and services, inquiries, orders, and customized solutions please visit:
Sirona Biochem Says SGLT Test Results Confirm Key ‘Breakthrough’
Last Updated on Friday, 9 October 2009 12:02 Written by Editor Friday, 9 October 2009 12:02
Sirona Biochem Corp. (TSX-V: SBM), an emerging biotech company focused on diabetes and obesity, says results of testing its unique SGLT inhibitor molecules demonstrate a key breakthrough milestone for Sirona Biochem.
Sirona Biochem CEO, Dr. Howard Verrico, said, “There are two vital steps in the early stage of drug testing: validation of concept i.e. a molecule is able to hit the desired target and secondly its in vivo effectiveness. This first round of testing has shown a key breakthrough milestone in the process of validating this concept.”
“The test results now mean we can proceed to find out whether the molecules are selective, safe and robust enough to have potential to be effective when they reach the parts of the body where the re-uptake of glucose needs to be limited.”
Dr. Bertrand Plouvier, Chief Scientist, said, “The results from the first round of screening are indeed very encouraging and Sirona Biochem will use the next following months to further study the molecules through specific assays to demonstrate their effectiveness and drug likeness.”
Dr. Verrico said management of sugar metabolism is a primary medical challenge associated with treating diabetes and obesity and that is why SGLT inhibitors show such promise in this regard. “At present SGLT2 inhibitors have demonstrated their ability to limit the re-uptake of glucose back into the blood stream from urine. However, they have been notoriously lacking in ability to resist being rapidly metabolized by the body, thus rendering them largely ineffective.
“What we have now done is show that our molecules, with their unique GlycoMim® technology, can inhibit the glucose transporter SGLT2. The next challenge, and an exciting one, is to show that our molecules are selective, safe and have the potential to have an increased efficacy compared to the current molecules undergoing clinical development.”
Sirona Biochem owns the worldwide product rights to a library of unique sodium glucose transporter (SGLT) inhibitors to treat diabetes and obesity. SGLT inhibitors, as previously stated, block the re-uptake of excess sugars from urine, which can then reduce high blood sugar towards normal levels.
Sirona Biochem has entered into a strategic partnership with TFChem, a drug discovery company based in Rouen, France. TFChem licenses its technology of fluorinated carbohydrate mimics: GlycoMim®, and products in development to biotech companies. This strategic partnership was completed by a detailed research and licence agreement signed on September 29, 2008.
23.6 million people, or 7.8% of the population of the United States, have diabetes. (February 2009 DACG.ORG)
Market Trends
In 2007, the prevention and treatment of diabetes and its complications was estimated to cost US$ 232 billion according to the International Diabetes Federation. By 2025, this is likely to increase to more than US$ 302.5 billion.
The diabetes drug market reached US$18 billion in 2005, and is expected to increase to $21-25 billion in 2011. With many new products yet to realise their full potential and the high incidence of T2DM expected in emerging markets, prospects for the sector look strong. Some of the fastest growing markets for diabetes are in emerging economies. India, China and Indonesia are in the top 5 for disease prevalence. The impact for both branded and generic drugs is considerable.
Furthermore, in recent years, obesity has become a major health problem for many post-industrial societies, so much so that in 2004, the United States Health and Human Services declared obesity to be a disease. The World Health Organization (WHO) projects that globally in 2005, 1.6 billion adults were overweight with at least 400 million adults obese. By 2015, approximately 2.3 billion adults will be overweight and 700 million will be obese. Obesity poses a major health risk because it greatly increases the risk of co-morbidities such as diabetes, cardiovascular diseases, arthritis, and cancer. Recognizing the potential for a new blockbuster market, major pharmaceutical companies have increasingly focused on obesity and its causes and, in the process, seeking to identify many potential targets and pathways that could be exploited to create novel therapies.
Sirona Biochem’s website is at: www.sironabiochem.com where we feature the most recent information about the company and its activities. Alternatively, investors are able to e-mail all questions and correspondence to info@sironabiochem.com where they can also request to be added to the investor e-mail list to receive all future press releases and updates or call John Dougherty, Corporate Development at 604-641-4466.
About Sirona Biochem
Sirona Biochem Corp. (TSX-V: SBM) is an emerging biotech company dedicated to the discovery and development of novel drug compounds. The current focus is on treatments for Type II diabetes and obesity. Sirona has entered into a license agreement with TFChem S.A.R.L., a drug discovery company based in Rouen, France. TFChem licenses its technology of fluorinated carbohydrate mimics: GlycoMim®, and products in development to biotech companies. The license agreement with TFChem provides for research and development of new compounds known as SGLT Inhibitors. SGLT inhibitors are a new and exciting class of compounds that have great promise and potential to treat both diabetes and obesity.
Mark Senner President and Director
Neither the TSX Venture Exchange nor its Regulation Services Provider (as that term is defined in the policies of the TSX Venture Exchange) accepts responsibility for the adequacy or accuracy of this release.
950-789 west pender street
vancouver, b.c., v6c 1h2
Direct: 604-641-4466
Fax: 604-608-5471
info@sironabiochem.com
Source: Marketwire
Agilux Laboratories Hires New Associate Director to Lead In Vitro ADMET Services Division
Last Updated on Thursday, 8 October 2009 12:22 Written by Editor Thursday, 8 October 2009 12:22
- Adrian Sheldon, Ph.D., Positions Contract Research Organization for Growth - WORCESTER, Mass.--(Business Wire)-- Agilux Laboratories, Inc., a Contract Research Organization (CRO) that provides bioanalytical and in vitro Absorption Distribution Metabolism Excretion Toxicology (ADMET) services for the biotechnology and pharmaceutical industries, has appointed Dr. Adrian Sheldon as associate director of In Vitro ADMET Services. In this role, Dr. Sheldon will build the In Vitro ADMET Services division offering testing services that allow biotechnology and pharmaceutical companies to screen drug candidates for desirable ADMET properties. Dr. Sheldon will leverage more than 17 years of industry experience, including establishing new business units for In Vitro ADMET and Immunochemistry within an established CRO. He will extend Agilux`s emphasis on customer service, rapid turnaround and exceptional data quality to the company`s newly formed In Vitro ADMET Services Testing Division. "We are excited to have someone with Adrian`s expertise, successful track record and demonstrated abilities at Agilux," said Jim Jersey, president and CEO at Agilux. "Adrian brings the right balance of scientific expertise and customer focus, which is consistent with Agilux`s mission of delivering high quality data at unprecedented speeds. We are confident that both the Agilux team and our clients will benefit from his unique skill set." Prior to Agilux, Dr. Sheldon served as associate director of In Vitro ADMET at Charles River Laboratories. Prior to Charles River Laboratories, Dr. Sheldon was group leader in Assay Development/HTS/In Vitro ADMET at ArQule where he co-managed a team responsible for screening compounds generated by the industry-leading combinatorial chemistry laboratory. He received his Ph.D. from Boston University and his A.B. from Harvard University. Dr. Sheldon has authored numerous scientific publications and holds two patents. "I am very pleased about joining the team at Agilux," stated Dr. Sheldon. "We have an incredible opportunity to change the way early stage development services are delivered and I am confident that I will be able to contribute to Agilux`s continuing success." About Agilux Laboratories, Inc. Agilux Laboratories, Inc. is a privately held contract research organization (CRO) focused on bioanlaytical and PK/PD testing services for the biotech and pharmaceutical industries. Leveraging industry and contract research experience of its management team, the company delivers high quality bioanlaytical chemistry and PK/PD data more rapidly. Agilux helps clients make better decisions during drug discovery and development by providing quality data earlier in the research process by using technologies and systems that increase turnaround speed well beyond industry standards. Founded in 2007 by industry experts Jim Jersey, Steve Guyan and Peter Glick, Agilux is headquartered in Worcester, MA and is funded by private equity firm, Ampersand Ventures. For more information, call 508-753-5000 or email sguyan@agiliuxlabs.com. Online at www.agiluxlabs.com. Agilux Laboratories, Inc. Steve Guyan Vice President, Sales and Marketing 508-762-4402 sguyan@agiluxlabs.com
Source: Reuters
Bayer CropScience invests EUR 4.9 million in compound logistics
Last Updated on Wednesday, 9 September 2009 10:31 Written by Editor Wednesday, 9 September 2009 10:31
7 Sep 2009 , Monheim : Bayer CropScience has invested EUR 4.9 million in the expansion of the compound logistics at its Monheim site. It has one of the most modern facilities in the world for storing chemical compounds. The company’s scientists use the 2.2 million or so substances currently in the collection to search for promising active ingredients for innovative crop protection products. After just 15 months of construction, the extension was inaugurated at a ceremony attended by Dr. Alexander Klausener, Head of Research at Bayer CropScience.
The purpose of the compound logistics is to store, prepare and distribute substances prior to comprehensive biological testing. “We are now in a position to pursue our research and development activities even more efficiently than before,†Dr. Klausener explained. With expenditures of EUR 649 million in research and development (2008), Bayer CropScience is one of the leading companies in its sector.
The central feature of the compound logistics, which has been extended to cover more than 1,000 square meters, is the substance storage area. The automatic miniload warehouse with some 24,000 storage positions now has space for about 7.6 million vials containing minute quantities of different chemical compounds. Placed side by side, the vials would cover a distance of around 161 kilometers. A total of 16 robots and retrieval units “work†in the facility, where they achieve a high throughput. They quickly supply researchers in Bayer CropScience’s institutes with the exact quantities they need; this spares resources and, above all, ensures “just in time†delivery. The investigational substances undergo a comprehensive screening procedure, in which they are tested to see whether they have a desired effect, for example in controlling fungal pathogens, insect pests or weeds, and could thus be suitable as the starting point for developing a new product.
About Bayer CropScience
Bayer is a global enterprise with core competencies in the fields of health care, nutrition and high-tech materials. Bayer CropScience AG, a subsidiary of Bayer AG with annual sales of about EUR 6.4 billion (2008), is one of the world’s leading innovative crop science companies in the areas of crop protection, non-agricultural pest control, seeds and plant biotechnology. The company offers an outstanding range of products and extensive service backup for modern, sustainable agriculture and for non-agricultural applications. Bayer CropScience has a global workforce of more than 18,000 and is represented in more than 120 countries. This and further news is available at: www.press.bayercropscience.com.
More information is available at www.bayercropscience.com
Posted under Compound Libraries, Compound Screening, Press Releases | No Comments
Baylor researchers find fat cell blocker
Last Updated on Tuesday, 8 September 2009 10:09 Written by Editor Tuesday, 8 September 2009 10:09
A small molecule that turns off the genes responsible for making fat cells has been discovered by a team of Baylor College of Medicine and Japanese researchers.
Dubbed “fatostatin,†the molecule blocks a protein in the cell that starts the cascade of events that turns on the 63 genes in the nucleus responsible for the generation of fat cells, said Salih Wakil, professor of biochemistry and molecular biology at BCM.
The report appears in the journal Chemistry and Biology.
“That is the exciting thing,†said Wakil. “This goes to the most basic level of the expression of genes that cause fat.â€
When mice with a predisposition to be obese received fatostatin, they lost weight, their cholesterol and fatty acid synthesis decreased. They had less resistance of insulin (a factor in diabetes), and their livers, which were pale because of fat buildup, returned to normal.
Drugs that lower cholesterol already exist, but they block only a single enzyme in the fat-generating pathway. Fatostatin stops the process at the beginning, said Wakil.
Wakil said one of his colleagues, Motonari Uesugi, now of Kyoto University in Japan, discovered the compound by screening a library of an estimated 10,000 compounds.
Lutfi Abu-Elheiga, associate professor of biochemistry and molecular biology at BCM was also a major contributor.
Source: bizjournals.com
Researchers develop screening test for cells that activate immune system
Last Updated on Wednesday, 26 August 2009 11:31 Written by Editor Wednesday, 26 August 2009 11:31
UT Southwestern Medical Center researchers are the first to design a large-scale, cell-based screening method that identifies which compounds activate immune-return cells that hold compact for prospective cancer-fighting vaccines.
The new screening technique can scan thousands and even millions of compounds to identify those that activate dendritic cells, which are on constant recon patrol throughout the body to scout out cancerous or infected cells and alert the immune system.
“Our assay is unique from other conventional ones in its sensitivity and cost- and time-efficiency,†said Dr. Akira Takashima, professor of dermatology and vice chairman for research and head of the project.
Dendritic cells (DCs) are considered key to developing future vaccines that can either mimic the body’s natural immune response or turn on immune responses that failed – due, for example, to cancer or an immune deficiency.
The team, which also included Dr. Norikatsu Mitzumoto, assistant professor of dermatology and the study’s lead author, and Drs. Hironori Matsushima and Hiroaki Tanaka, postdoctoral researchers in dermatology, created the cell-based biosensor system.
“We basically engineered DCs to express a fluorescent signal only when sensing activation signals so that you can identify immuno-stimulatory agents very easily,†said Dr. Takashima. Immuno-stimulatory agents launch the immune system.
The research appears on Blood magazine’s online Web site and will appear in a future issue.
“We have optimized the high-throughput screening capability – an experienced scientist can now test one thousand chemicals a day almost single-handedly,†added Dr. Mizumoto. Previously, scientists would have to test each compound individually, a time-consuming process.
Their research already has led to the discovery of several compounds that turn on dendritic cells, which are found throughout the body from skin to blood. They continuously scan the body at the cellular level looking for antigens – foreign cells and materials invading the body – and for molecular signatures of tissue damage or infection.
“Their primary job is to present antigens to the immune system so that you develop protective immunity for infection and cancer,†said Dr. Takashima.
The DC biosensor system should help pharmaceutical and biotech companies sift through large numbers of chemicals for ones that tell the dendritic cells to launch the immune response. It may also prove useful in identifying biothreat agents because it detects infectious pathogens with high sensitivity.
Dr. Takashima said he hopes to garner additional funding to discover potent immuno-stimulatory drugs by screening high-quality libraries of compounds.
Doing so may be the first step toward developing a new class of vaccines that force or trick the natural immune system to kick on, or initiate an immune response that can be copied and initiated artificially.
Other UT Southwestern researchers from dermatology involved in the study were Dr. Yasushi Ogawa, postdoctoral researcher, and Dr. Jimin Gao, former instructor.
The research was funded by the National Institutes of Health, the Dermatology Foundation Career Development Award and the American Cancer Society Junior Investigator Award.
http://www.utsouthwestern.edu/
TimTec Expands Partnership With Collaborative Drug Discovery Through Publishing Three Additional Libraries on CDD’s Free Public Access Database
Last Updated on Wednesday, 13 May 2009 03:56 Written by admin Wednesday, 13 May 2009 03:56
Last October, TimTec and Collaborative Drug Discovery (CDD) established a collaboration in which CDD’s web-based data management system would host two TimTec Natural Products libraries on their free community Public Access site.  Through this partnership, researchers would be able to register for a free account with CDD allowing them to chemically mine the contents of these TimTec compound libraries using CDD’s powerful, intuitive web-based database software.
TimTec is now offering three more libraries on the CDD Public Access database:
The TimTec ActiTarg-K Kinase Modulators library contains over 6,000 compounds known to inhibit protein kinase activity:
http://www.timtec.net/actitarg-k-kinase-modulators.html
The TimTec OGT Inhibitors Analogs library contains more than 300 compounds analogous to three known O-GlcNAc Transferase inhibiting molecules:
http://www.timtec.net/o-glcnac-transferase-inhibitors.html
Finally, the TimTec resourceful Diversity Set is a general screening collection of drug-like compounds that present most diversified selection from TimTec stock. This screening library contains 10,000 of the most diverse compounds, all complying with the Lipinski Rule of Five:
http://www.timtec.net/diversity-set-10k.html
TimTec’s five databases join more than 25 other databases containing chemical and biological data hosted on CDD Public Access, including:
- 47,000 Ki values for 20,000 compounds against 699 GPCR targets from the NIMH Psychoactive Drug Screening Program at the University of North Carolina
- Over 15,000 compounds with Malaria assay data from 5 public data sources
- 48,818 compounds from the Distributed Drug Discovery (D3) at Indiana University – Purdue University Indianapolis (IUPUI)
- Almost 7,500 compounds with Tuberculosis antibacterial and cell viability information from 4 public data sets and growing thanks to their collaboration with the Bill & Melinda Gates Foundation
About TimTec, LLC.
TimTec LLC. – http://www.timtec.net – is a privately held company located in NewarkDelaware, USA. It was founded in 1995 and began its work in the areas of acquisition and distribution of synthetic organic and natural compounds, custom synthesis, and laboratory equipment to become a full service partner for drug discovery. TimTec has established a global network of thousands of scientists from research centers around the world. The company has developed strong in-house expertise assembling general and targeted library collections for variety of research purposes. International customers include major pharmaceutical, biotech, agricultural, and educational companies and institutions, which use TimTec products for research and development programs.
For more information on TimTec library collections, please contact:
Kay Denisova
Business Development
TimTec LLC
Harmony Business Park Building 301-A
Newark, DE 19711
Tel 302 292 8500
Fax 302 292 8520
info(at)timtec.net
http://www.timtec.net
About Collaborative Drug Discovery, Inc.
Collaborative Drug Discovery, Inc. (CDD) – http://www.collaborativedrug.com – provides web-based software that organizes preclinical research data to help scientists advance new drug candidates more effectively. The CDD database enables scientists to “archive, mine, and collaborateâ€Â® around preclinical chemical and biological drug discovery data through a web-based interface. The software helps distributed research groups to safely store and intelligently analyze small molecule, enzyme, cell and animal bioactivity data accumulated from both low-throughput and high-throughput screens. Unique collaboration features and CDD’s community-oriented approach help unite globally dispersed humanitarian efforts against neglected infectious diseases. Similar collaborative strategies are also rapidly gaining prominence in the commercial arena. CDD offers its industrial-strength database software at a price affordable to academic laboratories, research foundations, and small companies.
For further information please contact:
Barry Bunin, PhD
President & CEO
Collaborative Drug Discovery (CDD)
1633 Bayshore Hwy, Suite 342
Burlingame, CA 94010
info(at)collaborativedrug.com
Posted under Compound Libraries, Diversity Libraries, North America, Press Releases, Targeted Libraries | No Comments
3rd International Symposium on Advances in Synthetic and Medicinal Chemistry
Last Updated on Sunday, 10 May 2009 10:19 Written by admin Sunday, 10 May 2009 10:19
Kiev, Ukraine, August 23 – 27, 2009
ASMC09 in Kiev is being prepared by EFMC (European Federation for Medicinal Chemistry) and ChemBridge Corporation, in the series of events which started with ASCMC04 Moscow followed by ASMC07 St. Petersburg.
Prof. Erick Carreira, ETH Zurich, Switzerland and Dr Scott Biller, Novartis Institutes for BioMedical Research, Cambridge, USA, have kindly accepted to be the Chairmen of the Symposium.
The scientific program of the International Symposium on Advances in Synthetic and Medicinal Chemistry will include:
* 28 invited plenary lectures, presented by highly recognized scientists from academia and the pharmaceutical and biotech industry from Europe, USA and former USSR countries.
* 10 short oral communications which will be selected from submitted abstracts
* poster sessions
The scientific program will be complemented by an attractive cultural program in Kiev.
The topics to be covered during this symposium include:
* New Synthetic Methodologies, Total Synthesis of Natural Products and Heterocyclic Chemistry
* Diversity- and Target-Oriented Synthesis and Chemical Biology
* Medicinal Chemistry and Drug Discovery & Development
The program will also include a commercial exhibition and a half-day Business Mini-Symposium “Small Molecule Screening Libraries in Drug Discovery: Experience and Trendsâ€.
The official language of the symposium is English.
http://www.ldorganisation.com
Plexxikon Receives Key Patents on Novel Compounds for Multiple Programs
Last Updated on Friday, 27 March 2009 10:00 Written by admin Friday, 27 March 2009 10:00
BERKELEY, Calif.–(BUSINESS WIRE)–Plexxikon Inc. today announced the issuance of key composition-of-matter patents covering novel compounds discovered through the company’s Scaffold-Based Drug Discoveryâ„¢ platform. Plexxikon’s pipeline of preclinical and clinical stage product opportunities currently span potential treatments for cardio-renal disease, CNS disorders, inflammation, metabolic disease and oncology. Two of the three recently issued patents (U.S. patents no. 7,498,342 and no. 7,504,509) cover compounds derived from the company’s discovery efforts to target protein kinases for the treatment of multiple indications including oncology and inflammation. The third patent (U.S. patent no. 7,476,746) covers novel compounds from the company’s PPAR (peroxisome proliferator-activated receptor) program yielding novel therapeutic opportunities for metabolic disorders and other diseases.
“We are pleased to be adding these additional patents to our growing and broad intellectual property portfolio,†stated K. Peter Hirth, Ph.D., chief executive officer of Plexxikon. “Plexxikon’s novel approach to drug discovery has enabled the company to advance multiple first-in-class drug candidates which are covered by strong intellectual property, and as a result, to secure significant pharmaceutical industry interest in our programs.â€
In contrast to fragment-based approaches, Plexxikon’s platform has generated multiple product opportunities by mining the relatively unexplored chemical space of scaffold-like cores and by utilizing co-crystallography early in the discovery process to guide chemical optimization of these scaffolds. Further, the company has developed methods to make highly selective kinase inhibitors as yet rarely seen. Plexxikon has demonstrated the ability to develop selectivity between two targets with as little as one amino acid difference in their catalytic domains. This capability has created the opportunity for the development of new targeted drugs not only for oncology, but also for chronic disease indications outside oncology where safety hurdles are even higher. To date, Plexxikon’s platform has led to the development of a targeted medicine for the treatment of melanoma, a drug candidate for polycystic kidney disease (PKD), an oral agent for rheumatoid arthritis and a broad spectrum oral diabetic therapeutic, all representing novel agents addressing significant unmet needs.
Dr. Prabha Ibrahim Promoted to Vice President of Chemistry
In other news, Prabha N. Ibrahim, Ph.D., was promoted to the position of vice president of chemistry, bringing over 15 years of experience to her position. As head of chemistry since 2002, she has played a key role in building the company’s synthetic and medicinal chemistry capabilities leading to the discovery of Plexxikon’s novel drug candidates now in the clinic and in preclinical development. Prior to Plexxikon, Dr. Ibrahim was a senior scientist at CV Therapeutics, where she was responsible for the identification and development of preclinical candidates for cardiovascular indications. She also previously worked at Amgen, where she played an integral role in small molecule drug discovery for inflammation therapeutics. Dr. Ibrahim earned her Ph.D. at the University of Victoria, Canada, and was a Welch Foundation Fellow at Rice University in Houston.
Plexxikon Profile
Plexxikon is a leader in the structure-guided discovery and development of novel small molecule pharmaceuticals to treat human disease. The company’s clinical stage programs include PLX4032 for the treatment of melanoma and colorectal cancer, PLX5568 for the treatment of PKD and PLX204 for the treatment of diabetes. Among the company’s preclinical development programs, candidates are being developed for the treatment of rheumatoid arthritis, multiple sclerosis and other autoimmune diseases.
Plexxikon’s proprietary Scaffold-Based Drug Discovery™ platform is being applied to build a pipeline of product opportunities in multiple therapeutic areas. This discovery process integrates multiple state-of-the-art technologies, including structural screening as one key component that provides a significant competitive advantage over other drug discovery approaches. To date, the company has discovered a portfolio of clinical and preclinical stage compounds in varied disease areas addressing significant unmet needs in each therapeutic category.
Plexxikon is seeking pharmaceutical and biotechnology partners for select collaboration opportunities. For more information, please visit www.plexxikon.com.
Salk Forms Stem Cell Partnership With Sanofi-Aventis
Last Updated on Friday, 27 March 2009 09:35 Written by admin Friday, 27 March 2009 09:35
The Salk Institute says it has formed a new stem cell research partnership with Sanofi-Aventis, the international pharmaceutical giant based in Paris. Financial terms of the five-year alliance were not disclosed, and some details of the deal remain to be worked out, Salk spokesman Mauricio Minotta told me this afternoon.
The Sanofi-Aventis regenerative medicine program will sponsor grants in promising research areas, and is intended to provide long-term, multi-participant collaborations between scientists at San Diego-based Salk and Sanofi-Aventis. “It’s meant to be a true collaboration, it’s not just funding,†says Michael White, who oversees the institute’s office of technology management and development. Sanofi-Aventis has about 16,000 employees in the United States, mostly at its U.S. headquarters in Bridgewater, NJ, and about 100,000 employees worldwide.
The program also will provide unrestricted support for the Salk Institute’s stem cell facility, which was created as a separate laboratory supported by private funding during the years the Bush Administration had placed restrictions on federal stem cell funding.
In a statement, Salk president William Brody says there are no preconditions concerning the collaborative alliance. “Our scientists will continue to freely explore cutting-edge research and publish their work,†Brody says. (That’s important to academic freedom, because companies have been known to try to squelch research findings if they don’t support the company’s marketing message.) Under this deal, Salk will also gain access to “extensive resources†at Sanofi-Aventis, which includes a large-scale facility in Tucson, AZ, for screening compounds with potential to be new drugs.
“That’s something that’s very attractive to us, to be able to screen our targets with their drugs,â€White says.
Such industry collaborations could be a sign of the times. In January, San Diego’s Burnham Institute for Medical Research announced a multi-year agreement with Johnson & Johnson’s Pharmaceutical Research and Development unit.
Source: xconomy.com
Posted under Collaborations, Compound Libraries, Compound Screening, Europe, North America, Press Releases | No Comments
Thermo Fisher Scientific Accelerates Drug Discovery Process With New Maybridge Quick2Leadâ„¢ Compound Kits
Last Updated on Friday, 27 March 2009 09:32 Written by admin Friday, 27 March 2009 09:32
Thermo Fisher Scientific, the world leader in serving science, announced recently that it has introduced a novel tool to accelerate hit-to-lead programmes in the drug discovery process. Its Maybridge Quick2Leadâ„¢ Compound Kits are designed to save time and money by enabling rapid compound library synthesis around bioactive “hits” emerging from screening assays. The kits are made up of pre-weighed, diverse building block selections, facilitating rapid capture of structure-activity (SAR) data from the closely related structural analogues within the library.
Quick2Lead Compound Kits are available as five functionality-based kits, with each one containing 48 carefully selected compounds. This enables the exploration of a wide area of chemical space to maximise credible SAR data acquisition for the successful conversion of an initial hit into a genuine, optimisable lead. Since these compounds are all pre-weighed, the kits are ready to use by simply adding solvent and transferring straight to a synthesiser.
The five functional groups available include: carboxylic acids, sulfonyl chlorides, amines, anilines and boronic acids. Each of these different functional groups is applicable to a wide range of tried and trusted parallel synthesis methodologies. Furthermore, although each kit taps into the hugely diverse Maybridge collection, they all include compounds from the top levels of the relevant Topliss Tree, thereby ensuring quality and rigour in interaction testing.
Each of the pre-selected compounds is supplied as 0.1mMol in a 5mL vial. This saves time and money at several levels — minimising stock, avoiding disposal and reducing storage footprint. The pre-selection process also avoids the “dead time” that can be experienced whilst waiting for multiple building blocks from internal and external sources. Maybridge Quick2Lead Kits arrive as a complete library, delivered rapidly ex-stock.
“Our aim with the Maybridge product range is to help shorten the discovery process, from screening to scale-up, and the introduction of our Quick2Lead Compound Kits is the latest addition to our broad product portfolio of pharmacophorically relevant compounds and services,” said Dr. Mick Durrant, Director of Business Development for Maybridge products at Thermo Fisher Scientific. “We recognise that identifying, sourcing and weighing building blocks to feed the library production process around an initial hit can be time consuming and expensive. Our new Quick2Lead Kits offer a novel approach to drive these costs down by providing pre-weighed, diverse building block selections which are simply ready-to-go.”
About Maybridge
Maybridge, part of Thermo Fisher Scientific, is well known for providing highly innovative drug-like molecules and screening compounds for drug discovery and development. With products available for both lab and development scale, they specialise in producing new heterocyclic and phenyl ring-based chemical building blocks, including a unique and expanding range of reactive intermediates.
About Thermo Fisher Scientific
Thermo Fisher Scientific Inc. is the world leader in serving science, enabling our customers to make the world healthier, cleaner and safer. With annual revenues of $10.5B, we have more than 34,000 employees and serve over 350,000 customers within pharmaceutical and biotech companies, hospitals and clinical diagnostic labs, universities, research institutions and government agencies, as well as environmental and industrial process control settings. Serving customers through two premier brands, Thermo Scientific and Fisher Scientific, we help solve analytical challenges from routine testing to complex research and discovery. Thermo Scientific offers customers a complete range of high-end analytical instruments as well as laboratory equipment, software, services, consumables and reagents to enable integrated laboratory workflow solutions. Fisher Scientific provides a complete portfolio of laboratory equipment, chemicals, supplies and services used in healthcare, scientific research, safety and education. Together, we offer the most convenient purchasing options to customers and continuously advance our technologies to accelerate the pace of scientific discovery, enhance value for customers and fuel growth for shareholders and employees alike.
SOURCE: Thermo Scientific Brand Products, Part of Thermo Fisher
Posted under Compound Libraries, Diversity Libraries, Drug-Like Compounds, Europe, New Products, Press Releases | No Comments
Conference focuses on potential new drugs for malaria, leishmaniasis, and trypanosomiasis
Last Updated on Thursday, 26 March 2009 09:52 Written by admin Thursday, 26 March 2009 09:52
A meeting in Colorado, USA has brought together chemists, biologists, pharmacologists, and clinicians in an attempt accelerate the discovery of new drugs for diseases caused by protozoan parasites. These include some of the major infectious diseases of poverty – malaria, leishmaniasis, human African trypanosomiasis and Chagas’ disease.
The organizers of the meeting, “Drug Discovery for Protozoan Parasites†held 22-26 March, point out that recent years have seen the welcome development of public-private research partnerships focused on diseases caused by protozoa – in most cases on malaria. However, these partnerships have mainly been concerned with translational research. As a result, several drugs have been advanced into clinical evaluation but, in the meantime, development of several apparently promising new drugs has not proved successful, “…thus leaving a sparse pipeline of new chemical entities that have potential for registration in the next few yearsâ€.
The objectives of the meeting were to discuss current methods to identify and validate new drug targets and to screen libraries of compounds to discover novel chemotypes; assess the potential for chemical biology and medicinal chemistry to optimize compounds that are specific and avoid resistance mechanisms; and identify critical paths for compound progression and to discuss the utility of key models for assessing preclinical drug leads.
Key problems addressed included identification and validation of new targets, chemical biology and medicinal chemistry approaches to characterize new compounds, novel screening techniques to identify new chemotypes, mechanisms of drug resistance, and cutting edge strategies to progress new drug candidates into clinical trials.
Several potentially important findings were reported. To give just one example, oral administration of an amphotericin B formulation, iCo-009, has been shown to have significant efficacy with no evidence of toxicity in mice infected with Leishmania donovani. Manufacturers iCo Therapeutics Inc, claim that “iCo-009 has overcome amphotericin B’s significant physicochemical barriers to absorption and holds promise for the development of a self-administered oral therapy for the treatment of visceral leishmaniasisâ€.
The meeting was supported by the Bill & Melinda Gates Foundation.
Posted under Compound Libraries, Compound Screening, Press Releases, USA and Canada | No Comments
EPA Presents Initial Results from Caliper Life Sciences’ ToxCast Screening Effort
Last Updated on Friday, 20 March 2009 04:59 Written by Editor Friday, 20 March 2009 04:59
HOPKINTON, Mass., March 19 /PRNewswire-FirstCall/ — Caliper Life Sciences, Inc. (NASDAQ: CALP) , a leading provider of tools and services for drug discovery and life sciences research, today announced that the United States Environmental Protection Agency (EPA) presented initial analyses of Phase I data generated by Caliper Discovery Alliances and Services (CDAS) under the EPA’s ToxCast(TM) screening program at the annual meeting of the Society of Toxicology (SOT) held this week in Baltimore, MD. Separately, the EPA notified Caliper that it has exercised the first additional option year under Caliper’s ToxCast contract with the EPA. Task orders under this contract have already generated approximately $3.5 million in total revenues for Caliper since the initiation of the contract in April, 2007, $1.2 million of which was recognized in 2008.
“We are pleased with the preliminary findings presented by the EPA,” said Kevin Hrusovsky, President and CEO of Caliper Life Sciences. “These results, coupled with the EPA’s third year option exercise, reinforce the likelihood for Phase II efforts to begin at Caliper in the third quarter of this year, which supports our expectation of receiving approximately $3 million of service task orders under this contract in 2009.”
Caliper works with the EPA under its ToxCast initiative to develop new in vitro (laboratory) approaches to identify chemicals that are potentially toxic to the environment. The initial phase of the EPA ToxCast program was aimed at creating a database of in vitro assay data on a broad set of compounds for which in vivo (animal) safety data already existed. Key goals for this phase were to assess overall data quality and establish that the database was predictive of in vivo toxicity profiles. Initial analyses of the data generated at CDAS indicate that the goals for high quality data and potential predictive power have been met. For the 11 replicate controls included in the initial 320 compound set, there was greater than 99% concordance in the screening results across 240 assays tested, and more than 200 correlations between the in vitro results generated at CDAS and in vivo toxicity parameters have already been identified. In addition, 75% of the assays tested showed activity for one or more compounds, reinforcing the need for broad in vitro profiling.
“We believe this data presentation validates the importance of in vitro profiling as a tool for predicting potential toxicity liabilities of compounds and highlights the high quality data generated by Caliper,” said David Manyak, Ph.D., Executive Vice President of Discovery Services at Caliper Life Sciences. “Our access to the entire Phase I ToxCast database makes Caliper an ideal partner for collaborative data mining projects. We also believe that the assay screening panel employed by Caliper for the ToxCast initiative will be broadly applicable for product development programs within the agricultural chemical and pharmaceutical industries.”
The ultimate goal of the ToxCast program is to develop a set of predictive in vitro assays that can supplement or replace in vivo tests currently used for regulatory approval of new environmental chemicals. If successful, the ToxCast initiative will reduce the cost and improve the speed of regulatory approval of new environmental chemicals. More extensive data analysis from the EPA is expected in mid-May of this year.
About Caliper Life Sciences
Caliper Life Sciences is a premier provider of cutting-edge technologies enabling researchers in the life sciences industry 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 translating 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 www.caliperLS.com.
Posted under Clinical Trials, Compound Libraries, North America, Press Releases | No Comments
Ligand Pharmaceuticals Inc. (LGND) Enters into Screening Agreement with Trevena
Last Updated on Thursday, 12 February 2009 04:00 Written by Editor Thursday, 12 February 2009 04:00
SAN DIEGO–(BUSINESS WIRE)–Ligand Pharmaceuticals Incorporated (NASDAQ:LGND – News) and Trevena Inc. today announced the initiation of a joint research and license alliance to screen targets using Trevena’s novel biological platform against Ligand’s combinatorial library of compounds, to identify active compounds with potential for development as novel G-protein coupled receptor (GPCR) therapeutics.
Under the terms of the agreement, Trevena has been granted exclusive worldwide rights to sublicense active compounds resulting from the collaboration. Ligand expects to screen 24 targets over two years and receive payments triggered by a tiered screening paradigm for each target.
“We are delighted to enter into this collaboration that allows us to generate cash flow from the combinatorial chemistry technology we gained through our acquisition of Pharmacopeia,” said John L. Higgins, President and Chief Executive Officer of Ligand. “Working closely with the Trevena team, we hope to rapidly identify and advance novel drug candidates using their unique insight into GPCR signaling pathways.”
Maxine Gowen, President and CEO of Trevena said, “We are excited to work with these exceptional scientists and get access to this proven chemistry platform. We believe that this collaboration will accelerate our drug discovery efforts and the validation of our biological platform.”
About Trevena, Inc.
Trevena, Inc. is a Philadelphia-based drug discovery company focused on developing pharmaceutical products targeting GPCRs. Pharmaceutical products that target GPCRs represent up to 40% of marketed drugs today. Trevena’s drug discovery platform, licensed from Duke University Medical Center, is based on extensive research from the laboratories of scientists Robert J. Lefkowitz, M.D. and Howard A. Rockman, M.D. The company’s drug discovery portfolio is currently focused on programs for cardiovascular and CNS indications. Trevena, Inc. is privately held. (www.trevenainc.com)
About Ligand Pharmaceuticals
Ligand discovers and develops new drugs that address critical unmet medical needs of patients with muscle wasting, frailty, hormone-related diseases, osteoporosis, inflammatory diseases and anemia. Ligand’s proprietary drug discovery and development programs are based on its leadership position in gene transcription technology. In December 2008, we acquired Pharmacopeia in a transaction that provides Ligand rights to numerous collaborations with pharmaceutical companies, pipeline programs and the world’s largest combinatorial chemistry library.
Posted under Collaborations, Compound Libraries, North America, Press Releases, Targeted Libraries | No Comments