Bio Screening Industry News

Potsdam, Germany and Allschwil, Switzerland (June 30, 2005) - Evolva Biotech SA (Allschwil, Switzerland) and AnalytiCon Discovery GmbH (Potsdam, Germany) announced today that they have entered into a strategic alliance to jointly apply their respective technologies to the generation and optimization of novel nuclear receptor agonists and related compounds.

Under the terms of the agreement Evolva will be responsible for the creation and optimization of nuclear receptor agonists using its Watchmaker® technology, as well as pre-clinical development. AnalytiCon will provide selected genetic and compound diversity through its MEGAbolite®-process, and will be responsible for compound de-replication, identification and scale-up.

Neil Goldsmith, Managing Director of Evolva, said “Watchmaker® is bringing a new paradigm in drug discovery. By bridging nature.s genetic diversity and chemistry with an evolution process it allows us to create small molecules optimized for specific therapeutic targets. Rather than to rely on nature to provide compounds of interest, we have designed a technology which evolves and delivers small molecules crafted for specific targets. We have already proven our approach can deliver novel, selective nuclear receptor agonists with desirable side-effect profiles. By securing a strategic collaboration with AnalytiCon, one of the leaders in modern natural product approaches, we recognize their expertise which complements judiciously our technology”.

Matthias Hess, Global Head of Marketing and Sales of AnalytiCon, commented “MEGAbolite® provides a cutting edge concept for the generation of pure natural products including state of the art fermentation, isolation and structure elucidation. MEGAbolite® is widely accepted in pharma industry for delivering new active principles based on biologically validated structures. We believe that the strategic collaboration with Evolva, which provides a proven and unique approach to generate new active compounds in the field of nuclear receptor agonists, will create a lot of synergies. Through this collaboration both partners will definitely leverage great technological and economical benefits. We are very pleased to enter into this strategic partnership with Evolva and we look forward to experience a bilateral success story.”

About Evolva
Evolva evolves small molecule drugs using massively combinatorial gene libraries that drive chemistry rich pathways. Its Watchmaker® technology platform replicates, on an industrial basis, the ability of nature to evolve molecules with exquisite “design”, but with the evolution directly aimed at making functional drugs - HIV blockers, anti-obesity compounds etc. Watchmaker® can create, optimize and manufacture molecules that are outside the scope of the traditional synthetic chemistry approaches of the industry. For further information see www.evolvabio.com

About AnalytiCon
AnalytiCon a brand and at the same time successful company, is world.s first address for all needs in connection with natural product drug discovery. >From prospecting for biosources, via fermentation, extraction and isolation to high throughput structure elucidation, the company provides a vast portfolio of first class services. Beyond that, AnalytiCon produces pure natural compound collections and libraries of synthetic, natural product based molecules carrying relevant bio-active structure elements. The natural product drug discovery platform is complemented by a portfolio of medicinal chemistry services. For further information see www.ac-discovery.com.

An indigenous Chinese herb similar to the popular garden sage in the West has been used to treat a variety of diseases since time immemorial.

It is called danshen, or Salvia miltiorrhiza in Latin.

Despite its popularity, Xuan Lijiang, a scientist at Shanghai Institute of Materia Medica (SIMM) under the Chinese Academy of Sciences, did not expect his research would herald a new wave in the study of traditional Chinese medicine (TCM) at the molecular level, when he took it up 13 years ago.

His assignment, along with his colleagues, was to study the chemical ingredients of the herbal plant.

A little more than a decade on, Xuan has been recognized for his contributions to the creation of an innovative drug that is licensed by the State Food and Drug Administration (SFDA).

The drug, called Depsides salts and extracted from the Chinese sage danshen, has also reportedly led dozens of institutes and pharmaceutical firms to launch research programmes to find effective molecules from other traditional medicines.

more…

GOTHENBURG, Sweden, June 28 /PRNewswire/ — Cellectricon proudly announces that AstraZeneca has implemented multiple Dynaflow systems on several sites worldwide. AstraZeneca’s integration of Dynaflow into their ion channel drug discovery program is an important validation of the system and proves its unique efficiency features.

Since the introduction of Dynaflow during fall 2003, AstraZeneca has placed several orders for the system and it is now used to meet their need for a cost efficient system. The Dynaflow system is built around a pioneering computer-controlled microfluidic chip used as tool by pharmaceutical companies to perform ion channel drug discovery with high speed and accuracy. The system enables novel ion channel experiments and offers less cost per data point since it gives uncompromised and pharmacologically relevant data at a high throughput. It also dramatically reduces the amount of reagent needed for testing. In August at the Drug Discovery Technology® & Development World Congress a new Dynaflow system will be launched. The system is designed to be used with any cell, any patch configuration, any active substance and any ion channel. The system comes with a new range of chips developed for safety pharmacology and offers maximum yield in hERG studies.

“There is a huge demand for efficient ion channel drug screening tools, but many solutions available today are costly and difficult to implement and manage,” says Ulf Jonsson, CEO of Cellectricon. “AstraZeneca’s decision to continuously invest in the technology is most gratifying and proves Dynaflow’s remarkable productivity increase and cost efficiency.”

“At AstraZeneca we have continued to invest in multiple Dynaflow systems because we find this to be the most flexible, increased throughput ion channel assay systems for use in whole-cell recording. It has allowed us to run experiments and screen compounds on ion channel targets not possible before this system and at a throughput previously inconceivable on these targets,” says Dr. Edwin C. Johnson, Director, CNS/Pain Research Area & Head, Target Biology Department at AstraZeneca R&D, Wilmington, Delaware, US. “We view the Dynaflow as an excellent investment and look forward to more ion channel screening products from Cellectricon.”

“The Dynaflow ™ system has substantially increased our throughput and reduced the amount of compound needed for testing,” says Dr. Ingemar Jacobson, who is Principal Scientist at AstraZeneca R&D in Molndal, Sweden. “The Dynaflow ™ technology is superior in most aspects when compared to other systems on the market.”

About Cellectricon

Cellectricon AB (Gothenburg, Sweden) develops life science tools based on world leading science competences. The products target bottlenecks in the drug discovery process. The first generation of products, Dynaflow ™, provides groundbreaking systems for ion channel drug discovery and offers dramatic productivity increase with major savings in both time and cost. The company was formed in 2000 based on an extensive and solid patent portfolio within different areas such as high-throughput electrophysiology, microfluidics, microfabrication, and electroporation. Cellectricon is a privately held company and the main shareholders are InnovationsKapital, Investor Growth Capital and Karolinska Investment Fund.

From: Select Biosciences Ltd

The agenda is now available for Select Conferences inaugural Ion Channel Targets conference and exhibition being held in Waltham, Boston, 20-21 September 2005. With easy worldwide access and inexpensive registration fees a high degree of interest is anticipated. Early registration is therefore recommended as delegate numbers will be limited.

We are delighted to announce a top quality agenda featuring 4 sessions and 20 speakers assembled from academia and industry. Chairing the first session, Ion Channels in Drug Discovery, is Dr. Michael Xie who is currently Associated Director of Biology at Synta Pharmaceuticals. On the afternoon of the first day Dr. Chris Mathes, Vice-President and General Manager of Sophion, will chair Advances in Ion Channel Technology and Screening. The second day will open with Ion Channels in Disease Biology chaired by our key note speaker Prof. David Clapham. He is currently Professor of Cardiovascular Research Investigator at the Howard Hughes Medical Institute and Professor of Neurobiology, Harvard Medical School. The meeting will close with Target Identification and Validation chaired by Dr. Maria Garcia, who is a Distinguished Senior Investigator in the Department of Ion Channels at Merck Research Laboratories.

In order to ensure the widest possible audience for our speakers registration fees start at just $399. So, if you want to see the latest research and equipment in ion channels whilst networking with your peers then this event is both affordable and unmissable.

Agenda

Day One 20th September

09:00 Ion Channels in Drug Discovery
Chaired by Dr. Michael Xie - Synta Pharmaceuticals

09:05 Combination Screening of Ion Channel Targets to Reduce False Positive Rate
Dr. Christopher Fanger, Hydra Biosciences

09:40 Ion Channel Targets in Drug Design for Cancer Therapeutics
Dr. Amit Banerjee, Wayne State University

10:15 Coffee and Networking in Exhibition

10:45 Novel Antagonists of Human Kv4.3: HT Ion Channel Screening in Transgenic C. elegans.
Dr. Andreas Kopke, Devgen nv

11:20 HERG, Repolarization and Sudden Cardiac Death
Dr. Arthur M. Brown, ChanTest, Inc.

11:55 Ion Channel Drug Discovery in Non-excitable Cells
Dr. Michael Xie, Synta Pharmaceuticals

12:30 Lunch and Networking in Exhibition

13:45 Advances in Ion Channel Technology and Screening
Chaired by Dr. Chris Mathes - Sophion Biosciences

13:50 Automated Patch Clamp Technology: Evaluation of QPatch® for Voltage Gated Na-channel Characterization
Dr. Mads Peder Gersdorff Korsgaard - Neurosearch

14:25 Utilising Ion Channel Cell Lines and High Throughput Electrophysiology in the Context of Drug Discovery and Development
Dr. Ray Helliwell, Cytomyx

15:00 Application of the Aequorin Assay Technology for Ion Channel Drug Discovery
Dr. Sandra Arpino, GlaxoSmithKline

15:35 Coffee and Networking in Exhibition

16:05 Cell Volume Cytometry: a new HTS
Dr. Susan Hua, University at Buffalo, SUNY

16:40 Using the Dynaflow System to Assess Novel Drug Properties at the 5HT3 Receptor
Dr. Geoffrey Tombaugh, Memory Pharmaceuticals Corp.

17:15 End of day
Informal cocktail reception hosted by Cytomyx at their facilities in Lexington, MA.

Day Two 21st September

09:00 Target Identification and Validation
Chaired by Dr. Maria Garcia- Merck Research Laboratories

09:05 Detection of Alternative Splicing Events in Ion Channels
Dr. Richard Einstein, ExonHit Therapeutics, Inc.

09:40 Identification and Validation of New Ion Channel Drug Discovery Targets
Dr. John Montana, Paradigm Therapeutics Ltd.

10:15 Coffee and Networking in the Exhibition

10:45 A High Throughput Mutation Screen of Human Ion Channel Genes in Common Inherited Neurological Disorders
Dr. Ronald G. Lafreniere, Emerillon Therapeutics Inc.

11:20 Quantitative Proteomics to Study Ion Channels in Brain
Dr. Jacek Wisniewski, Protana Inc.

11:55 Identification of novel classes of Kv1.x-Kvß1 channel modulators
utilizing protein-protein interaction assays
Dr. Rachel Ginham - University of Bristol

12:30 Lunch and Networking in Exhibition

13:45 Ion Channels in Disease Biology
Chaired by Prof. David Clapham

13:50 Ion Channels and Innate Immunity in Human Disease
Dr. Jatinder Ahluwalia, University College London

14:25 TRP Ion Channels as Drug Targets
Prof. David Clapham, Aldo R. Castañeda Professor of Cardiovascular Research, Investigator, Howard Hughes Medical Institute & Professor of Neurobiology, Harvard Medical School

15:00 CLIC4 as a Novel Target for Tumor Therapy
Dr. Kwang Suh, NIH/ NCI/ Center for Cancer Research

15:35 Coffee and Networking in Exhibition

16:05 Agonism of the Trp-p8 Ion Channel for the Treatment of Cancer
Dr. Sateesh Natarajan, Dendreon Corporation

16:40 Mechanosensitive Ion Channel Inhibitors: a new class of drugs
Prof. Frederick Sachs, University at Buffalo, SUNY

17:15 Close of Conference

ChemDiv and AdipoGenix Extend Discovery and Medicinal Chemistry Collaboration

SAN DIEGO, and BOSTON, June 23 /PRNewswire/ — ChemDiv, Inc. and AdipoGenix, Inc. have announced that AdipoGenix has been awarded a SBIR grant from NIDDK for a collaboration with ChemDiv to further progress small molecules that target human fat tissue as therapy for obesity and type 2 diabetes. ChemDiv supplies AdipoGenix with specific small molecule compound libraries, medicinal and custom chemistry services to support AdipoGenix’s unique biology for discovering compounds that reduce fat content of human fat cells and identifying mechanisms of action and molecular targets for active compounds.

“Our screening collaboration with ChemDiv has produced a promising lead compound with exciting mechanism of action and molecular target,” said Dr. Gerri Waloga Vice President of AdipoGenix. “This grant award supports the lead optimization stage of our ChemDiv collaboration with the goal of achieving candidates for IND-enabling preclinical development.”

“We are very pleased that AdipoGenix has selected ChemDiv as its partner on the grant to utilize ChemDiv’s strong drug discovery chemistry expertise for development of a new drug to treat obesity”, said Dr. Ilya Okun, VP of R&D at ChemDiv, Inc. “Having an extensive experience in innovative small molecule synthesis and medicinal chemistry, we are confident that this partnership will lead to a successful fulfillment of the project goals” — he continued.

About ChemDiv, Inc.

ChemDiv Inc. (ChemDiv) is a global chemistry-driven contract research organization focused on the delivery of new scientific innovation and products and services that meet the drug discovery needs of its partners. ChemDiv provides partners with access to Discovery Outsource(TM) a full service drug discovery capability encompassing; medicinal chemistry; pre-clinical development; synthetic chemistry; diverse & focused screening libraries, global logistics. For additional information, please visit http://www.chemdiv.com/

About AdipoGenix Inc.

AdipoGenix is a Boston-based biopharmaceutical company developing pharmaceuticals that target human fat tissue to treat obesity and its co-morbidities, including diabetes and cardiovascular disease. Through its proprietary human fat cell-based technology, AdipoGenix identifies nontoxic, small molecule compounds that reduce the fat content in human fat tissue, which is expected to provide therapeutic benefit for these important diseases. http://www.adipogenix.com/

ChemDiv, Inc.

CONTACT: Natalie Ikizalp of ChemDiv, Inc., +1-858-794-4860; or EdCannon, President and CEO of AdipoGenix Inc., +1-617-638-5660; or Kari Lampkaof MacDougall Biomedical Communications, +1-508-647-0209,klampka@macbiocom.com, for AdipoGenix Inc.

Web site: http://www.adipogenix.com/

Web site: http://www.chemdiv.com/

High Throughput In Vitro Multiple Readout Screens Expected to Reduce Development Time of New Therapies

Serologicals Corporation (NASDAQ: SERO) today announced that Upstate Group, its wholly owned subsidiary, has initiated a collaboration with CXR Biosciences to establish a battery of proprietary in vitro screens to select, at an early stage, candidate molecules for further development. The underlying principle of the platform is to enable the identification of compounds with the most optimal safety or bioavailability profiles as early in the drug development process as possible. The result of this will be to advance molecules most likely to succeed into clinical development, thereby reducing the overall time-to-market of life-enhancing therapies. The screening platform will utilize predictive toxicity and drug metabolism screens to profile compounds in various cell-based and in vitro assays.

Dr Tom Shepherd, Chief Executive of CXR commented “As a significant part of the tremendous costs involved in drug development are expended on drugs that fail during the development process, not only should this platform improve the quality of candidate drugs entering the clinic, but it should also improve the cost effectiveness of the overall process. Perhaps most importantly, this platform is intended to reduce the time-to-market of critical new life-enhancing therapies.”

Upstate is the leading research discovery provider of cell signalling products and services to the life science market. Its customers are biomedical researchers at drug discovery companies and academic institutions in the key disciplines of oncology, immunology, proteomics, cardiology and neurology. Known for its enabling, innovative solutions to help understand the biology of kinases, chromatin, G-proteins and cytokines, Upstate’s advanced cell biology tools - drug screening services, enzymes, state-specific antibodies, siRNA kits, multiplex assays - are used by thousands of customers worldwide to accelerate the discovery and development of new therapeutic compounds.

David A. Dodd, President and Chief Executive Officer, Serologicals commented “The cost of successfully developing and commercialising new pharmaceuticals is now approximately $1 billion, requiring more than a decade of development and regulatory review. The result of our collaboration with CXR Biosciences is intended to contribute to a significant reduction in both the cost and development time of new pharmaceutical compounds, enabling biopharmaceutical companies to focus more quickly on those development projects with the highest likelihood of success. This collaboration, combined with our existing leadership in providing drug discovery profiling solutions, will further expand our growth in this strategic area of our business.”

Upstate is a leading research discovery provider of the highest quality cell signaling products and services to the life science market. Its customers are biomedical researchers at drug discovery companies and academic institutions in the key disciplines of oncology, immunology, proteomics, cardiology and neurology. Known for its enabling, innovative solutions to help understand the biology of kinases, chromatin, g-proteins and cytokines, Upstate’s advanced cell biology tools - drug screening services, enzymes, state specific antibodies, siRNA kits, multiplex assays are used by thousands of customers worldwide, every day to accelerate improving human health. Upstate, a Serologicals company, is headquartered in Charlottesville, VA, with locations in Lake Placid, NY, and Dundee, Scotland.

For more information, please visit our website www.upstate.com.

CXR Biosciences is a drug development solutions company which is applying new models for pre-clinical drug development, and the assessment of risks to humans of chemicals, that are aimed at introducing new dimensions in the capacity to make predictions about safety in humans in a more rapid and informed manner. The Company was co-founded by Professor Roland Wolf FRSE, FRB Med Sci, FSA and Dr. Cliff Elcombe. Professor Wolf is Director of the University of Dundee Biomedical Research Centre, and Honorary Director of the Cancer Research UK Molecular Pharmacology Unit. He has published over 350 papers in peer-reviewed scientific journals and has recently received the Gerhard Zbinden Award for his extensive contributions to the area of drug and chemical safety. Dr. Cliff Elcombe is a Senior Lecturer in the Biomedical Research Centre, University of Dundee Medical School. He has authored or co-authored over 100 peer-reviewed publications and previously had a highly successful career in investigative toxicology at Zeneca. CXR applies a combination of extensive experience in conventional models for the evaluation of drug metabolism and toxicity. CXR’s customers and collaborators include 8 major pharmaceutical companies and over 20 small drug discovery companies.

CXR Biosciences Ltd is located in Dundee, Scotland.

For more information, please visit our website: www.cxrbiosciences.com.

Serologicals Corporation (NASDAQ: SERO), headquartered in Atlanta, GA, is a global leader in developing and commercializing consumable biological products, enabling technologies and services in support of biological research, drug discovery, and the bioprocessing of life-enhancing products. Our customers include researchers at major life science companies and leading research institutions involved in key disciplines, such as neurology, oncology, hematology, immunology, cardiology, proteomics, infectious diseases, cell signaling and stem cell research. In addition, Serologicals is the world’s leading provider of monoclonal antibodies for the blood typing industry.

Serologicals employs a total of more than 1,000 people worldwide in three Serologicals’ companies: Chemicon International, headquartered in Temecula, CA, Upstate Group, LLC, headquartered in Charlottesville, VA and Celliance Corporation, headquartered in Atlanta, GA.

For more information, please visit our website: www.serologicals.com.

This release contains certain forward-looking statements within the meaning of the Private Securities Litigation Reform Act of 1995. Words or phrases such as “should result,” “are expected to,” “we anticipate,” “we estimate,” “we project” and similar expressions are intended to identify forward-looking statements. These statements are subject to certain risks and uncertainties that could cause actual results to differ materially from those expressed in any forward-looking statements. These risks and uncertainties include, without limitation, our ability to continue to introduce new products at a rapid pace and the acceptance of such products by our customers.

Serologicals is a registered trademark of Serologicals Royalty Company.

CONTACT:

Serologicals Corporation Public Affairs Bill Davis, 678/728-2018

Potential new drugs for neurological disorders like Parkinson’s are being screened faster thanks to world-leading CSIRO software that automatically assesses a drug’s effect on nerve cells.

The image analysis software will be highlighted at BIO2005, the world’s largest biotechnology conference, on 19-22 June in Philadelphia, USA.

In the search for new pharmaceuticals, thousands of chemical compounds are screened to see if they’re effective and safe.

CSIRO’s software is being used to find new treatments for neurological disorders by measuring nerve cell changes faster and more thoroughly than other commercially available software - this means thousands of samples can be screened in a day.

The CSIRO software is now in software toolkits for several high content screening instruments, with German company Evotec Technologies announcing its CSIRO licence last month.

CSIRO’s Pascal Vallotton says that cell counting and allocating neurites to individual cells is traditionally done manually.

“Nerve cells have very complex branches, like a tree. For a person to work out which branches belong to which cells and then measure changes due to the drugs being tested is difficult and slow”, he says.

“Not only that, different technicians will usually give different answers”.

The CSIRO software can also be used in high content screening instruments because it can automatically analyse cell changes in an instant.

These instruments capture and process images of the cells, giving critical measurements that help pharmaceutical companies decide which compounds to investigate further.

“With this kind of resource at their fingertips, it will be easier to find treatments for diseases”, says Dr Vallotton.

http://www.csiro.com.au

Researchers at the University of Kansas and the University of Kansas Medical Center have won an almost $8 million National Institutes of Health contract to find chemical compounds to develop into reversible male contraceptives that do not rely on steroids or affect bodily hormones.

Science & TechnologyLawrence, Kan. - infoZine - The five-year contract will allow the scientists from the two campuses to continue research and testing started in partnership with the NIH four years ago that has led to the development of promising chemical compounds. The KU team is one of only a few research groups in the world working to develop male contraceptives.

“We are in partnership with the NIH to develop chemical compounds that can eventually be turned into safe, effective and reversible male contraceptives,” said Gunda Georg, lead researcher on the project. “The NIH awarded this research contract to us because of the interdisciplinary and collaborative nature of our team, as well as the technology and laboratories KU and KUMC have for testing.”

Georg is also director for the Center for Drug Discovery at the Higuchi Biosciences Center on the Lawrence campus. The other primary members of her team are Joseph Tash, associate professor of molecular and integrative physiology at KUMC; Qi-Zhuang Ye, research professor at the Higuchi Biosciences Center; and Ernst Schonbrunn, assistant professor of medicinal chemistry.

In its work under the previous NIH contract, the KU team identified a chemical compound they named Gamendazole that caused temporary infertility in male rats by affecting sperm production, Georg said. Gamendazole, on which KU has filed a patent application, emerged from more than 100 compounds tested.

“The KU team has identified a dose of Gamendazole that caused 75 percent of the rats to lose fertility in week three after taking the compound and 100 percent of the rats to become completely infertile in week four and five,” Georg said. “Partial fertility begins to return to the rats in week six.”

The group also focused on finding novel inhibitors of key enzymes that either have an important role in sperm development or motility, Georg said. Finding chemical compounds to temporarily deactivate the enzymes so that the sperm do not fully develop or cannot move to cause pregnancy is the key objective of the research.

“We need to find compounds that are potent, selective and can be developed to be taken orally,” said Tash. “We do not want a compound to affect other enzymes in the body. We want to specifically target the right enzyme and nothing else.”

As part of the new NIH contract, hundreds of thousands of compounds will be tested on the key enzymes to see which ones might affect them. About 100,000 of those compounds will come from KU. The NIH will supply the rest.

KU was able to win the contract, in part, because of the research facilities available at the university, including the High Throughput Screening Laboratory, under the direction of Ye and a part of the Life Sciences Research Laboratories at 1501 Wakarusa Drive. While High Throughput Screening (HTS) technology is more common in private industry, KU is one of the few universities in the nation to have one, Georg and Schonbrunn said. Without the HTS lab, screening hundreds of thousands of compounds could take up to a year, but with the technology, screening time is dramatically reduced.

All the testing of compounds to date has taken place with rats and in test tubes. In the case of Gamendazole, human clinical trials could take place in three to four years with the approval of federal regulators.

“Through our research, we now know a great deal more about the male reproductive system,” Tash said. “We know what we might be able to do in this area and what enzymes we can target. The science has come to the point that we can say with some confidence that a reversible male contraceptive can be developed.”

Award is part of NIH effort to empower public sector to speed up medical discoveries

By Lisa Rossi, Pitt Chronicle

Pitt’s School of Medicine has received $9 million from the National Institutes of Health (NIH) to establish the University of Pittsburgh Molecular Libraries Screening Center (UP-MLSC).

The center is one of nine in the nation that will create the most sophisticated methods for rapidly assessing hundreds of thousands of compounds for their biological activities and therapeutic potential—a capability that has until now been limited almost exclusively to pharmaceutical companies. Moreover, to help speed the use of promising targets for drug development, all information collected by the centers will be freely available to the entire scientific community through PubChem, a comprehensive database that has been established by NIH.

As part of NIH’s Roadmap, which has as its overarching theme “New Pathways to Discovery,” NIH has allocated $88.9 million over the next three years to create the Molecular Libraries Screening Centers Network (MLSCN). NIH selected nine outside institutions as pilot centers to be included in the network, as well as NIH’s Chemical Genomics Center. Each center will work to develop the necessary tools conducting so-called high throughput screenings of molecules—which by the third year will allow each center to screen up to 100,000 molecule compounds using 20 different approaches, or assays, that help determine how these compounds interact with molecular targets, within cells, and are involved in regulating events that may be the root cause of different diseases.
Pitt’s center takes advantage of close ties between the School of Medicine’s Department of Pharmacology and the School of Arts and Sciences’ Department of Chemistry, along with new facilities devoted to drug discovery in the newly constructed Biomedical Science Tower 3. It also represents a unique collaboration with neighboring Carnegie Mellon University and with Sandia National Laboratories in Albuquerque, N.M., and provides the UP-MLSC unique expertise in design and development of novel probes that use fluorescence and other optical imaging techniques.

John S. Lazo, the Allegheny Foundation Professor of Pharmacology in Pitt’s medical school and principal investigator of the UP-MLSC, said: “As a pilot center in the Molecular Libraries Screening Centers Network, we will be able to exploit and expand our existing strengths for developing and implementing methods for the detection, characterization, and refinement of small molecules that have attractive biological and pharmacological properties and may eventually be further developed as therapeutic approaches to treating various diseases and conditions.”

Lazo will direct a core of UP-MLSC devoted to assay implementation. Andreas Vogt, research assistant professor of pharmacology in Pitt’s School of Medicine, will focus on high throughput screening, exploiting Pitt’s existing expertise in screening compounds in the context of whole cells. Peter Wipf, University Professor in Pitt’s Department of Chemistry and coprincipal investigator, will lead the new center’s synthetic chemistry core; the focus of that core will be to further improve and refine compounds designated as being the most promising to better target the specific errors that occur on the smallest of scales yet have profound effects on the development of disease. Mark D. Rintoul, manager of computational biology at Sandia National Laboratories, will direct UP-MLSC’s informatics core.

An NIH steering committee for the MLSCN, of which Lazo will be a member, will determine which of the most promising methods for screening molecules will be pursued and select from among its network of funded pilot centers those that will develop and implement these particular assays.

The National Institutes of Health (NIH) today announced it is awarding $88.9 million in grants to nine institutions over three years to establish a collaborative research network that will use high-tech screening methods to identify small molecules that can be used as research tools. Small molecules have great potential to help scientists in their efforts to learn more about key biological processes involved in human health and disease.

“This tremendous collaborative effort will accelerate our understanding of biology and disease mechanisms,” said Elias A. Zerhouni, M.D., NIH Director. “More importantly, it will, for the first time, enable academic researchers to explore novel ideas and enable progress on a broad front against human disease.”

For example, the broad-based screening effort will eventually enable researchers to explore the hundreds of thousands of proteins believed to be encoded by the approximately 25,000 genes in the human genome. To date, only a few hundred human proteins have been studied in detail using small molecule probes.

Certain small organic chemical compounds, also referred to as small molecules, can be valuable tools for understanding the many important cellular events involved in health and disease, which is key to identifying possible new targets for diagnosis, treatment and prevention. To date, most useful small molecules have been found serendipitously. The molecular libraries screening program is an effort by NIH to take an efficient, high-throughput approach toward the discovery of many more useful compounds.

The Molecular Libraries Screening Centers Network is being developed through the NIH Roadmap for medical research. Specifically, the network is part of the Roadmap’s “New Pathways to Discovery” initiative, which has set out to advance the understanding of biological systems and build a better “toolbox” for medical researchers in the 21st century. The network is funded by all of the institutes of the NIH and co-administered by the National Institute of Mental Health (NIMH) and the National Human Genome Research Institute (NHGRI) on behalf of NIH. The operation of the network will be overseen by a project team made up of staff from NIH’s 27 institutes and centers.

Data generated from the high-throughput assays conducted at the screening centers will be made available to researchers in both the public and private sectors through the PubChem database (http://pubchem.ncbi.nlm.nih.gov/), created and managed by the National Library of Medicine at NIH. The network’s first screening center, the NIH Chemical Genomics Center (NCGC), was established in June 2004 by the NHGRI’s intramural program to jumpstart the roadmap effort. Another critical component of the network is the Molecular Libraries Small Molecule Repository, located in San Francisco at Discovery Partners International, a drug discovery research firm. The repository houses the collection of small molecules that will be used for screening by the centers. Already, the repository has acquired nearly 100,000 compounds that are being utilized by the NCGC.

“This new Screening Centers Network will be the engine of discovery in the NIH Roadmap Molecular Libraries initiative,” said NIMH Director Thomas R. Insel, M.D. “Using the compounds from the Molecular Libraries Small Molecule Repository and supported by the informatics capabilities of PubChem, the MLSCN should provide researchers with many new chemical tools to explore how cells function at the molecular level.”

“This collaborative screening effort will enable academic and government researchers to contribute in a much more vigorous way to an understanding of the mechanisms of disease, and even to the identification of potential targets for new therapies. Central to this effort are the databases supporting the network, which will allow us to tie together data from diverse fields of science in ways not previously brought to bear on important health problems,” said NHGRI Director Francis S. Collins, M.D., Ph.D.

The nine institutions receiving grants as part of the Molecular Libraries Screening Centers Network (MLSCN) are:

* Columbia University Medical Center, New York, New York; James Rothman, Principal Investigator; MLSCN Center at Columbia University
* Emory University, Atlanta, Georgia; Raymond Dingledine, Principal Investigator; Emory Chemistry-Biology Center in the MLSCN
* Southern Research Institute, Birmingham, Alabama; Gary Piazza, Principal Investigator; Southern Research Molecular Libraries Screening Center (SRMLSC)
* The Burnham Institute, La Jolla, California; John Reed, Principal Investigator; San Diego Chemical Library Screening Center
* The Scripps Research Institute, La Jolla, California; Hugh Rosen, Principal Investigator; Scripps Research Institute Molecular Screening Center
* University of New Mexico Albuquerque, Albuquerque, New Mexico; Larry Sklar, Principal Investigator; New Mexico Molecular Libraries Screening Center
* University of Pennsylvania, Philadelphia, Pennsylvania; Scott Diamond, Principal Investigator; The Penn Center for Molecular Discovery
* University of Pittsburgh at Pittsburgh, Pittsburgh, Pennsylvania; John Lazo, Principal Investigator; University of Pittsburgh Molecular Libraries Screening Center
* Vanderbilt University, Nashville, Tennessee; C. David Weaver, Principal Investigator; Vanderbilt Screening Center for GPCRs, Ion Channels, and Transporters

About NIH
The National Institutes of Health (NIH) — The Nation’s Medical Research Agency — is comprised of 27 Institutes and Centers and is a component of the U. S. Department of Health and Human Services. It is the primary Federal agency for conducting and supporting basic, clinical, and translational medical research, and investigates the causes, treatments, and cures for both common and rare diseases. For more information about NIH and its programs, visit www.nih.gov.

About the NIH Roadmap for Medical Research
The NIH Roadmap is a series of new initiatives designed to pursue major opportunities and gaps in biomedical research that no single NIH institute could tackle alone but which the agency as a whole can address to make the biggest impact possible on the progress of medical research and to catalyze changes that will serve to transform new scientific knowledge into tangible benefits for public health. Additional information about the NIH Roadmap can be found at its Web site, www.nihroadmap.nih.gov.

About NIMH and NHGRI
NIMH and NHGRI co-lead the Molecular Libraries Roadmap Initiative and are among the 27 institutes and centers at NIH. NIMH works to reduce the burden of mental illness and behavioral disorders through research on mind, brain, and behavior. Additional information about NIMH can be found at its Web site, www.nimh.nih.gov. NHGRI supports the development of resources and technology that will accelerate genome research and its application to human health. Information about NHGRI can be found at its Web site, www.genome.gov.