Bio Screening Industry News

Bethesda, MD, December 12, 2009 –(PR.com)– James A. Wells, professor and chairman of the department pharmaceutical chemistry at the University of California, San Francisco, and director of UCSF’s small molecule discovery center, has been named the winner of the 2010 American Society for Biochemistry and Molecular Biology-Merck Award for his pioneering studies in the field of protein engineering.

Wells, who also serves on the ASBMB Council, will present an award lecture, titled “Probing and Controlling Cellular Remodeling Enzymes,” at 2:15 p.m. Monday, April 26, at the 2010 annual meeting in Anaheim, Calif.

Wells integrates multiple disciplines, including biophysics, cell biology, chemical biology, molecular biology, enzymology and proteomics, to design small molecules and proteins that can selectively activate or inhibit cellular processes such as differentiation and apoptosis. Through these efforts, Wells hopes to better understand how signaling events drive responses, such as cell growth and death, and perhaps discover new drugs to treat diseases like cancer.

Along the way, Wells has developed numerous innovative methodologies to improve protein engineering, molecular screening and pharmaceutical chemistry, including a disulfide-based protein-trapping technology, substrate-assisted catalysis and N-terminomics.

“[Wells] is an exciting and highly creative scientist,” noted Ian A. Wilson, professor of structural biology at The Scripps Research Institute, “and these methods that he has pioneered have been invaluable to countless researchers in a multitude of fields.”

“His unbridled enthusiasm is infectious and ensures his lab is fully regaled with a plethora of ideas,” Wilson continued, “so they can unleash their individual talents to further progress drug discovery, biochemical mechanisms, protein function and understanding of key cellular events that impact human health.”

Wells’ impressive expertise in protein engineering stems from a long and renowned career in the pharmaceutical industry. Before joining UCSF, Wells spent nearly two decades at Genentech Inc., where he was a founding scientist of its protein engineering department. He later founded and served as president and chief scientific officer of Sunesis Pharmaceuticals and helped invent a novel drug-discovery platform called Tethering, which efficiently screens molecules to identify the most potent compounds that block specific protein action.

Prior to that, Wells received his bachelor’s degree in biochemistry from the University of California, Berkeley, in 1973 and his doctorate in biochemistry from Washington State University in 1979. He also took on postdoctoral fellowships at both Washington State University and the Stanford University School of Medicine before joining Genentech in 1982.
his career, Wells has made enormous contributions to our understanding of enzyme mechanisms, allostery, protein plasticity, protein-protein interfaces, small molecule discovery, hormone receptor signaling, molecular recognition, protease signaling and apoptosis,” said Molecular and Cellular Proteomics co-editor Alma Burlingame, who is also a professor of chemistry and pharmaceutical chemistry at UCSF. “Not only has his science led to fundamental discoveries, it also produced new products in both the industrial enzyme and pharmaceutical sectors.”

The ASBMB-Merck Award, presented annually, recognizes outstanding research contributions in the fields of biochemistry and molecular biology.

Source: pr.com

AUSTIN, Texas — Dr. Jennifer Brodbelt, professor of chemistry and biochemistry at The University of Texas at Austin, has received a $734,068 grant from the National Institutes of Health (NIH) to develop a new method for rapidly screening blood samples for biomarkers.

Biomarkers are small molecules that indicate the presence of a particular physiological condition, typically a disease. The new method, if successful, could prove useful not just for identifying markers of specific diseases such as cancer or heart disease, but for discovering broader metabolic patterns correlated with conditions such as aging or obesity.

“There are technologies right now that are very effective at separating and analyzing the different compounds in a blood sample, but they tend to be relatively slow,” says Brodbelt, the principal investigator of the grant. “It makes it very hard to do analyses of lots of samples. What we’re developing is a chip-based method, where entire classes of compounds are captured on the chips and then all the compounds are released and analyzed by mass spectrometry in just a few seconds.”

Although the technology, if successful, should be useful in searching for biomarkers in all sorts of conditions, Brodbelt and her collaborators from Southwestern University in Georgetown, Texas, Drs. Lynn and Frank Guziec, are focusing on patterns that correlate with aging.

“We’re trying to develop maps that can correlate the progression of aging with metabolites that might be circulating in your blood,” says Brodbelt. “These could be small molecules that increase in quantity as you age, or actually change in composition as one ages.”

The new method, says Brodbelt, involves three basic stages.

The first stage is the coating of different regions of a mesh chip with a variety of “capture agents,” which chemically bind to specific compounds in a blood sample. A burst from an ultraviolet light then severs the chemical bonds between the chip and the captured substances. Then an electrospray, which is similar to a solvent aerosol spray, shoots through the mesh chip and transfers the different compounds into the mass spectrometer for analysis.

By analyzing the mass spectrometric data, says Brodbelt, scientists should be able to measure the presence and quantity of different compounds, and to do so on a scale, and with a speed, that wasn’t possible before.

“The payoff could be big,” she says. “It’s a different strategy than what might be pursued by molecular biologists or biochemists. They’ll often focus on studying one or two proteins at a time, and develop a really deep understanding of those proteins. We’re looking for the more generalized profile, and we may notice some patterns that weren’t apparent to them.

“There are so many other areas where you’d want to do profiling. It might involve looking for pesticides as part of an environmental study, or doing protein-related work or drug profiling work. If this approach is successful, I imagine other groups will try to develop these chips as well.”

Brodbelt’s grant, which is being funded as part of the American Recovery and Reinvestment Act (ARRA) government stimulus package, is a “Challenge Grant,” meant to encourage high-risk, high-reward research projects that may produce results quickly.

This is the second NIH grant in two years that Brodbelt and the Guziecs have received. In 2008, the collaborating groups received a four-year, $1,113,615 grant to evaluate an innovative technique that could assess the anti-cancer activity of new compounds.

For more information, contact: Jennifer Brodbelt, Department of Chemistry and Biochemistry, 512-471-0028.

Trana Discovery and Southern Research Institute Find Bioactive HIV Antiviral Compounds: NIAID contracts additional $700,000 to screen 300,000 more compounds for HIV inhibition

PRNewswire - October 28, 2009
CARY, N.C. and BIRMINGHAM, Ala., Oct. 28 /PRNewswire-USNewswire/ — Trana Discovery, Inc., an infectious disease drug discovery technology company, and Southern Research Institute, a not-for-profit contract research organization conducting basic and applied preclinical drug research, today announced that several bioactive hits from a set of 15,000 diverse small molecule compounds screened under contract with the National Institute of Allergy and Infectious Diseases (NIAID) exhibit antiviral activity against HIV-1 infected cells. Among the compounds tested at Southern Research using the Trana HIV 201 High-Throughput Screening (HTS) assay, 16 compounds demonstrated inhibition of HIV replication in infected human cells and several of these compounds were judged to be “potentially druggable.”

The screening assay used to identify the compounds is based on the premise that HIV-1 has evolved to use tRNALys3 as a primer for initiation of reverse transcription. Therefore, the interaction between tRNALys3 and viral genomic RNA represents a potential novel target for HIV-1 drug development. The biochemical assay to identify inhibitors of the interaction between tRNALys3 and HIV-1 genomic RNA was developed by Trana and transferred to Southern Research for high-throughput screening. Southern Research converted the assay to a homogeneous amplified luminescent proximity assay using AlphaScreen(R) reagents from PerkinElmer.

During this initial pilot study, 164 compounds were identified from the diversity set library as hits. Of these hits, 136 were retested in dose-response against HIV-1IIIB replication in a CEM-SS cytoprotection assay. Sixteen of this last group of compounds inhibited HIV-1 replication.

“These data indicate that the TRANA Discovery assay has identified a number of compounds with modest antiviral activity against HIV-1,” said Roger Ptak, Co-Principal Investigator, Southern Research Institute, in his report to the Division of Acquired Immunodeficiency Syndrome (DAIDS) within NIAID. “Additional testing of compounds with similar structures, as well as broader HTS, should lead to the identification of lead compounds that inhibit HIV-1 replication through the novel mechanism of inhibiting the interaction between tRNALys3 and viral genomic RNA.”

As a result of this successful pilot study, DAIDS has approved $700,000 of additional funding for the contract with Southern Research Institute in order to screen an additional 300,000 compounds and to conduct confirmatory testing of selected lead compounds. Lead candidates (or analogs) identified through this screening will be pursued by Trana Discovery for development and to secure the property rights and patents as deemed appropriate.

Toward that end, Trana Discovery is seeking organizations interested in licensing identified leads or that hold diverse collections of compounds or compounds with known bioactivity against HIV but unknown mechanism of action to identify candidates for drug development.

The use of high-throughput screening (HTS) assays developed by Trana Discovery can provide licensing opportunities for exclusive rights to new drug classes and reduce the cost and time for drug discovery.

“We are excited about the results from the initial screening efforts and for the confidence exhibited by the NIAID/DAIDS by this additional funding commitment,” said Steve Peterson, CEO of Trana Discovery. “We remain very optimistic that the use of our HIV assay will lead to new antivirals for the treatment of this disease.”

NIAID conducts and supports research to study the causes of infectious and immune-mediated diseases, and to develop better means of preventing, diagnosing and treating these illnesses. The NIAID is a component of the National Institutes of Health (NIH), the primary federal agency for conducting and supporting basic, clinical and translational medical research. Work for this project was performed under the DAIDS, NIAID contract N01-AI-70042; Roger Miller, Project Officer.

The HTS screening was conducted at the Southern Research High-Throughput Screening Center which consists of a suite of laboratories designed for efficient screening of large compound libraries and has the capacity for screening a wide variety of assay types. The Trana Discovery assay was recently validated in a 1536 well format, which increases the screening capabilities to over 100,000 compounds per day.

Organizations interested in licensing the Trana HIV 201 assay should contact Trana at info@tranadiscovery.com or by calling 866-390-3452 (toll free) or +1-919-342-6192. Parties interested in screening compounds using this assay at Southern Research Institute facilities may contact David Harris at d.harris@southernresearch.org or call +1-800-967-6774.

About Trana Discovery, Inc.

Trana Discovery, an anti-infective drug discovery technology company, helps its partners find new classes of drugs for the treatment of serious bacterial, viral, and fungal infectious diseases. Our proprietary assays identify compounds that work through a unique mechanism of action: inhibition of the target pathogen’s ability to use transfer RNA (tRNA) essential for propagation. The use of high-throughput screening assays developed by Trana Discovery will reduce the cost and time for drug discovery. Our assays provide licensing opportunities for exclusive rights to new drug classes. Trana Discovery has licensed the patented technology emanating from 20 years of research conducted at North Carolina State University, and holds patents that expand on this core technology and its use in high throughput screening. The company is located in Cary, North Carolina. For more information, please visit www.tranadiscovery.com.

About Southern Research Institute

Southern Research Institute is a nonprofit 501(c)3 scientific research organization that conducts preclinical drug discovery and development, and advanced engineering research in materials, systems development, environment and energy. Our more than 550 scientific and engineering team members support clients and partners in the pharmaceutical, biotechnology, defense, aerospace, environmental and energy industries. Southern Research is headquartered in Birmingham, Ala., with facilities in Wilsonville, Ala., Anniston, Ala., Frederick, Md., and Durham, NC and offices in New Orleans, La., Washington, DC and Kiev, Ukraine. For more information about Southern Research and its capabilities and accomplishments, visit www.SouthernResearch.org.

*Bilbille Y, et al. Vendeix Nucleic Acids Res. 2009 Jun;37(10):3342-53. Epub 2009 Mar 26. See www.tranadiscovery.com for complete reference.

Source: Southern Research Institute

BIRMINGHAM, Ala. - (Business Wire) DiscoveryBioMed, Inc. (DBM) today announced that it has been awarded a Phase 1 Small Business Innovation Research (SBIR) grant by the National Institutes of Health (NIH). The $308,000 grant will be used to advance certain small molecule drug discovery programs designed to correct the genetic mutation most common to cystic fibrosis (CF). “SBIR funding is an essential part of DiscoveryBioMed’s ability to provide our academic clients with cost-effective access to our world-class drug discovery engine,” said Dr. Erik Schwiebert, Chief Executive Officer of DiscoveryBioMed. “By screening our test drugs on DBM’s proprietary disease-relevant human cell backgrounds, our clients are able to facilitate their basic research, bringing new therapies closer to patients. The SBIR grant announced today is an example of this strategy in action.”

Dr. Schwiebert continued, “We are particularly pleased that the NIH has chosen to provide funding for this important drug discovery program and we are proud to be partnered with UAB’s Gregory Fleming James Cystic Fibrosis Research Center in the pursuit of new clinical treatments for Cystic Fibrosis.”

To date, DiscoveryBioMed, along with partners, James Collawn, Ph.D. and Zsuzsa Bebok, M.D., have screened approximately 25,000 compounds as part of this program. As a result of the SBIR award announced today, the team will be able to screen 50,000-70,000 additional compounds. In addition, the collaboration has already yielded the discovery and validation of a panel of 5 lead corrector compounds with nanomolar potency and 10-20 fold greater potency that any existing corrector drugs. Medicinal chemistry derivatives are currently being synthesized from the most potent lead compound from a family of drugs that had common molecular structure. Patent protection is in its final stages with work being facilitated by the UAB Research Foundation.

DBM and UAB investigators have mutual rights to existing and future lead compounds going forward and have contributed equally to the partnership.

“We are extremely pleased to be working with DiscoveryBioMed. Their exceptional technology and excellent small molecule screening library make them an ideal partner for this program, said James F. Collawn, Ph.D., Professor of Cell Biology at UAB. “We look forward to a continued and active scientific collaboration with DiscoveryBioMed.”

Dr. Collawn continued, “The SBIR grant announced today is a meaningful endorsement of our efforts investigating novel approaches to the development of therapies for the treatment of patients with CF. We believe the human airway epithelial cell model, which was acquired and licensed by DiscoveryBioMed, expressing the mutant CFTR from an endogenous gene is currently the best model for studies of this type. The funds made available through the SBIR grant will allow us to explore new ideas regarding mutant CFTR rescue and may lead to treatment alternatives for CF patients in the near future.”

The grant announced today is the second to be awarded to DBM this year. The previous award, announced in September, was a Phase 2 SBIR grant to continue research into the discovery and development of small molecules to alleviate multiple chronic human diseases.

About DiscoveryBioMed, Inc.

DiscoveryBioMed, Inc. is a life sciences and biotechnology company that engages in R&D and services work in cell engineering and production and cell-based drug discovery. The company is located within Innovation Depot in Birmingham. Using physiologically relevant cell culture models preferably derived from normal and diseased adult human cells and tissues, it focuses on finding therapeutic compounds for a variety of human diseases. It also applies this custom human cell-based approach to its “fee-for-service” support to researchers in allied areas and currently serves clients both locally in Alabama as well as in 11 other states in the US currently. For more information, visit the DBM website at www.discoverybiomed.com.

Discovery BioMed, Inc.
Erik Schwiebert, Ph.D., 205-307-6535 x 1
erik@discoverybiomed.com
or
Red Mountain Communications
Jonathan M. Nugent, 205-566-3026
jnugent@redmtncom.com

Source: earthtimes.org

Appenzell, Switzerland, October 19, 2009 / b3c newswire / - ERGONEX Pharma received one of the prestigious ‘European Orphan Diseases Entrepreneurial Company Award’ on the occasion of Frost & Sullivan’s ‘2009 Excellence in Healthcare Awards Banquet,’ held in London on 8th October 2009. The highly competitive award was presented to ERGONEX Pharma in recognition of the company’s innovative therapeutic concept, its impressive display of technological know-how and targeted vision.

ERGONEX Pharma is focused on the clinical development and commercialisation of Terguride for the treatment of distinct orphan diseases. Terguride is currently being evaluated for the treatment of pulmonary arterial hypertension (PAH) in a Phase II trial in Europe and headline results are expected in 2010.

Dr. Rudolf Reiter, CEO of ERGONEX Pharma comments: “This award comes at an exciting and challenging time for ERGONEX Pharma. I see it as recognition of the vision, the commitment and work of the company, which would not have been possible without the continued support, expertise and out-of-the-box thinking of our partners in the on-going clinical trial. We believe that Terguride has the potential to contribute a new quality to emerging combination therapies for patients, who do not tolerate, have become resistant to or are insufficiently controlled by current treatment options in PAH.”

The Frost & Sullivan Healthcare Awards Banquet honours Europe’s best healthcare companies for their achievements over the course of this year. Frost & Sullivan’s highly competitive awards recognise companies in a variety of regional and global markets for demonstrating outstanding achievement and superior performance in areas such as leadership, technological innovation, customer service, and strategic product development.

Link to the news release

About Pulmonary Arterial Hypertension
Pulmonary arterial hypertension is a disorder of the blood vessels in the lung, in which the pressure in large blood vessel rises above normal. Walls of the blood vessels are thickened and hardened, becoming less elastic. Hence, the decrease in lumen leads to increases in pressure. Patients with PAH suffer from extreme shortness of breath as the heart struggles to pump against these high pressures causing such patients to ultimately die of heart failure.

About Terguride
Terguride acts as a potent antagonist on 5-HT_2B and 5-HT_2A receptors: It has anti-proliferative and anti-fibrotic activities and drives reverse remodelling processes. Serotonin is a signal molecule in the body with many functions. In the blood vessel walls of the lung, it stimulates proliferation of smooth muscle cells and narrowing of the blood vessels, which has been implicated in PAH. Furthermore, trophic effects of serotonin on the heart contribute to right heart hypertrophy and progression towards heart failure. Terguride is approved in Japan for hyperprolactinemia acting as a partial dopamine agonist on the pituitary gland.

About ERGONEX Pharma - www.ergonex.com
ERGONEX Pharma is a pharmaceutical company focused on developing and commercialising well-tolerated and effective products for novel and typically underserved indications. This is being achieved by forging collaborations with commercial and academic partners with expertise in the field of interest and through outsourcing activities to service providers.

Contact
ERGONEX Pharma GmbH
Ruetistr. 20
CH-9050 Appenzell
Switzerland
Phone: +41 71 788 4065
E-mail: info@ergonex.com
www.ergonex.com

Bicoastal effort could help revolutionize the search for new therapies

La Jolla, CA, and Jupiter, FL, October 5, 2009 –A pair of scientists from The Scripps Research Institute, one on each coast, has been awarded a five-year $3.9 million grant from the National Institutes of Health (NIH) to develop a new technology to accelerate the search for new protein ligands – compounds that bind to proteins and alter their function.

Current screening technology, which is slow and expensive, has caused what the NIH calls a “major bottleneck” in the search for these basic tools that are key for the broader study of biological processes and that lay the groundwork for development of most drugs.

The grant, awarded as part of the NIH’s new Roadmap Transformative R01 Program, will be shared between the laboratories of Tom Kodadek, Ph.D., a professor in the Scripps Research Departments of Chemistry and Cancer Biology in Jupiter, Florida, and Benjamin Cravatt III, Ph.D., professor and chair of the Department of Chemical Physiology and member of The Skaggs Institute for Chemical Biology and Helen L. Dorris Child and Adolescent Neuro-Psychiatric Disorder Institute at Scripps Research in La Jolla, California.

“Ben and I are extremely pleased to win this highly competitive award and to be among the first selected for the new Transformative Grant program from the NIH,” Kodadek said. “This is a perfect example of the tremendous collaborative possibilities available within Scripps Research. We worked on the proposal together and the fact that we’re both part of the same national institution will make the work that much easier as we move ahead.”

Cravatt added, “This project is a good reflection of what those of us at Scripps Research in La Jolla and in Florida are trying to accomplish – fostering collaborative interaction and working on complimentary research projects. This will help cement the strong working relationship between our two campuses.”

The NIH Roadmap Transformative R01 (T-R01) Program awards were launched this year to support exceptionally innovative, high risk, original, and/or unconventional research projects that have the potential to create or overturn fundamental scientific paradigms.

“The appeal of the Pioneer, New Innovator, and now the T-R01 programs, is that investigators are encouraged to challenge the status quo with innovative ideas, while being given the necessary resources to test them,” said NIH Director Francis S. Collins, M.D., Ph.D. “The fact that we continue to receive such strong proposals for funding through the programs reflects the wealth of creative ideas in science today.”

Two Innovative Methods and a Cab Ride

The new Scripps Research project will combine two separate technologies from each laboratory – a peptoid library synthesis and screening platform developed in the Kodadek laboratory and an activity-based protein profiling system developed in the Cravatt laboratory.

Kodadek’s screening platform involves the creation of vast libraries of peptoids (peptoids are synthetic molecules that are similar to peptides, compounds that when joined together make up proteins) displayed on microscopic beads that are screened against fluorescently tagged proteins that light up after binding with a high affinity, highly selective ligand.

“Our screening technology simulates the cellular environment,” Kodadek said, “because the tagged proteins, which represent only a small fraction of the total, are mixed in with un-tagged competitors. There is a specificity filter built into the process from the beginning.”

The Cravatt Laboratory has pioneered the Activity-Based Protein Profiling technology, which allows scientists to identify protein classes based on their activity. The basic technology attaches a single label or probe to proteins from a particular subset of the proteome, which allows access to what are considered low abundance proteins and makes it ideal for massive parallel screening experiments. So far, Activity-Based Protein Profiling probes have been developed for more than a dozen distinct enzyme classes.

Cravatt’s technology makes it possible to target what he calls “interesting classes of proteins” but in a highly parallel fashion – hundreds of screens at a time of those multi- million member peptoid libraries. Although both scientists have known one another for some time, many of the details of the collaboration were worked out on a cab ride from England’s Heathrow airport to London last summer.

“Tom and I had an editorial board meeting in London, and shared a cab from the airport,” Cravatt said. “The fact that Tom had recently joined Scripps Florida helped get us energized about the project.”

“It’s true,” Kodadek added. “The ideas behind the grant proposal just popped out of that ride.”

A Transformational Marriage

The combination of the Kodadek and Cravatt advanced technologies will allow the screening of massive peptoid libraries (1-10 million synthetic compounds) in parallel fashion, a novel strategy that the scientists predict will increase the rate of ligand discovery by several hundred times over current methods.

“The gist of our proposal is quite simply marrying these two beautifully worked out technologies,” Kodadek said. “We have a good track record on both sides, plus we’re building off these innovative platforms, so if this works, and I’m certain it will, it will definitely be transformational.”

That transformation, when it comes, should result in more lead drug candidates, Kodadek said, because while the scientists’ success rate has been lower than those using current high throughput screening technology, the quality of the ligands identified has been significantly better. Some of this is due to the fact that simple synthetic compounds like peptoids have many advantages over other ligands such as antibodies. They can be modified easily for attachment to surfaces and can be produced in relatively large amounts at lower cost and rather quickly – a multi-million member peptoid library, for example, can be created in around three days.

“The way most science works today,” Cravatt said, “is that researchers tend to huddle around those areas where there are tools available. By combining our technologies, we will have a streamlined, unbiased way to identify high quality protein ligands and that will give us access to a large part of the proteome that others can’t study right now because the current technology is inadequate.”

About The Scripps Research Institute

The Scripps Research Institute is one of the world’s largest independent, non-profit biomedical research organizations, at the forefront of basic biomedical science that seeks to comprehend the most fundamental processes of life. Scripps Research is internationally recognized for its discoveries in immunology, molecular and cellular biology, chemistry, neurosciences, autoimmune, cardiovascular, and infectious diseases, and synthetic vaccine development. Established in its current configuration in 1961, it employs approximately 3,000 scientists, postdoctoral fellows, scientific and other technicians, doctoral degree graduate students, and administrative and technical support personnel. Scripps Research is headquartered in La Jolla, California. It also includes Scripps Florida, whose researchers focus on basic biomedical science, drug discovery, and technology development. Scripps Florida is located in Jupiter, Florida.

Source: eurekalert.org

BioLeap and GSK have entered into an agreement whereby BioLeap will design novel
lead compounds for "difficult" drug targets. The targets (not disclosed) are
ones for which conventional approaches, like high throughput screening, have
failed to yield a viable chemical starting point. Typically these are in areas
of high unmet medical need.

BioLeap will use its computational fragment-based drug design platform to
conceive compounds de novo that are molecularly tailored to bind to the target.
GSK will synthesize and test the compounds in biochemical and cellular assays.
The process will iterate until GSK selects a Lead Candidate. The terms of the
agreement for services were not disclosed.

David Pompliano, PhD, CEO of BioLeap said, "We are very pleased to be working
with GSK to accelerate the discovery of truly novel medicines. BioLeap`s
platform reliably predicts the effect of compound modifications on target
affinity, thus minimizing unproductive guesswork during drug discovery, and
producing a better drug candidate more quickly."

About BioLeap

BioLeap is a leader in computational fragment-based drug design. The company`s
proprietary design technology and process successfully addresses one of the
biggest problems in pre-clinical drug discovery: the limitation of drug like and
patentable leads for important biological targets. BioLeap is using its
completely "in-silico" platform to quickly and accurately predict
fragment-protein binding information that provides drug designers new insights
that enable them to efficiently create new and improved drug molecule
candidates. The BioLeap computational approach addresses the time, cost, and low
probability of success limitations imposed by traditional library screening and
lead optimization methods. BioLeap is utilizing its capabilities to advance its
own internal preclinical stage programs while collaboratively enabling
non-competing programs with numerous pharmaceutical partners.

Source: reuters.com

National Cancer Institute Chemical Biology Consortium to coordinate academic, private and government cancer drug discovery efforts

BIRMINGHAM, Ala., Aug. 20 /PRNewswire-USNewswire/ — Southern Research Institute today announced that it has been selected as one of 11 organizations to help establish the National Cancer Institute’s (NCI) Chemical Biology Consortium (CBC)–a program meant to coordinate and accelerate the discovery and development of new therapeutic agents to treat cancer patients. Southern Research will establish one of NCI’s five Comprehensive Chemical Biology Centers at its Birmingham campus.

“We are very pleased that Southern Research was selected to participate in this new program to expedite and coordinate the discovery and development of new cancer therapies,” said W. Blaine Knight, Ph.D., vice president of Drug Discovery and Principal Investigator of this effort at Southern Research. “Cancer accounts for nearly one out of every four deaths in this country and the National Institutes of Health estimate that the overall costs of cancer last year were more than $228 billion for health expenses and lost productivity. The search for newer and better drugs is never-ending, and something cancer patients and their families depend upon.”

Southern Research has a remarkable cancer-fighting track record having already discovered six FDA-approved drugs currently used in the treatment of cancer–amifostine, fludarabine, dacarbazine, lomustine, carmustine and clofarabine–with seven additional drugs in late stage preclinical and early clinical trials. Scientists at Southern Research have also evaluated approximately 50 percent of all FDA-approved cancer drugs currently available for patients.

“Our experience in cancer research and our track record in drug discovery were clearly recognized by our selection as a Comprehensive Center in the CBC consortium,” said John A. Secrist III, Ph.D., president and CEO of Southern Research. “We look forward to partnering with the federal government as it accelerates cancer drug discovery.”

As a Comprehensive Chemical Biology Center, Southern Research will focus on numerous aspects of preclinical drug research from target discovery, assay development, high throughput screening, structural/computational chemistry, and biology, through lead optimization and preclinical development. In addition Southern Research has an extensive compound library that will be made available for the CBC effort.

Dr. Knight says that work is expected to begin immediately.

This project has been funded in whole or in part with Federal Funds from the National Cancer Institute, National Institutes of Health, under Contract No. NO1-CO-12400. The content of this publication does not necessarily reflect the views or policies of the Dept. of Health and Human Services, nor does the mention of trade names, commercial products or organizations imply endorsement by the U.S. Government.

About the Chemical Biology Consortium

The CBC will establish an integrated network of chemical biologists, molecular oncologists, and compound screening centers from government, academia, and eventually from industry. The drug discovery strategy of the CBC is to expand current NCI programs by providing a coordinated focus on therapeutic opportunities in high-risk, under-represented areas, significantly advancing the discovery of novel compounds active against specific molecular and genetic cancer targets. CBC efforts will include recruiting extramural investigators with specialized expertise in novel discovery platforms as well as medicinal chemistry, chemical biology, molecular oncology, and other areas of drug discovery and development. The CBC will be centrally managed to coordinate the selection of targets and screening for agents that interact with these targets, and will then use an iterative development process to design and optimize drug “hits” into “leads.” The CBC will benefit from access to the NCI’s late-stage drug development resources and expertise.

The program is being developed by NCI’s Division of Cancer Treatment and Diagnosis (DCTD), in conjunction with NCI’s Center for Cancer Research (CCR) and the NCI Director’s Office, with guidance from external advisory panels. This effort will be managed by the NCI’s Experimental Therapeutics (NExT) Program. SAIC-Frederick, Inc. (SAIC-F) will provide support for the key operational and technical aspects. It is envisioned that this Consortium will provide cutting-edge chemical tools for probing complex biochemical signaling pathways and will serve as the starting point for the elaboration of first-in-class targeted therapies. The long-term vision of the CBC is to bridge the gap between basic scientific findings and NCI-supported clinical research to facilitate the discovery and development of new agents to treat patients with cancer.

Participants will have an unparalleled opportunity to participate in a highly collaborative drug discovery partnership with the National Cancer Institute (NCI). Using state-of-the-art communication, data-sharing and project management tools, the CBC will effect a paradigm shift in the use of public-private partnerships to translate knowledge from leading academic institutions into ground-breaking new drug candidates for patients with cancer.

About Southern Research Institute

Southern Research Institute is a nonprofit 501(c)3 scientific research organization that conducts preclinical drug discovery and development, and advanced engineering research in materials, systems development, environment and energy. Our more than 550 scientific and engineering team members support clients and partners in the pharmaceutical, biotechnology, defense, aerospace, environmental and energy industries. Southern Research is headquartered in Birmingham, Ala., with facilities in Wilsonville, Ala., Anniston, Ala., Frederick, Md., and Durham, NC and offices in New Orleans, La., Washington, DC and Kiev, Ukraine. For more information about Southern Research and its capabilities and accomplishments, visit www.SouthernResearch.org.

Vanderbilt University has been selected as one of 10 centers in the nation to participate in the Chemical Biology Consortium (CBC), a major new initiative to facilitate the discovery and development of new agents to treat cancer.

As one of four Chemical Diversity Centers, Vanderbilt’s role in the consortium will be to synthesize and optimize new compounds as potential cancer therapeutics.

“This is a real tribute to our growth in cancer chemistry and the leverage between the Vanderbilt Institute of Chemical Biology (VICB) and the Vanderbilt-Ingram Cancer Center (VICC),” said Lawrence Marnett, Ph.D., the Mary Geddes Stahlman Professor of Cancer Research and director of the VICB.

Alex Waterson, Ph.D., research assistant professor of Pharmacology and director of the VICB’s Chemical Synthesis Core, will lead efforts developing small molecule drug candidates. Gary Sulikowski, Ph.D., Stevenson Professor of Chemistry and a co-director of the core, will direct projects involving natural products.

Designed to accelerate the discovery and development of effective, first-in-class targeted therapies, the CBC will choose high-risk targets that are of low interest to the pharmaceutical industry. The CBC is a National Cancer Institute initiative administered by contractor SAIC-Frederick, Inc.

“It’s exciting in the sense that, right off the bat, (the NCI) said that the goal of this program is to develop drugs for cancer treatment,” said Sulikowski. “They’re looking for unique targets, unique approaches, and they think that academia may offer that.”

“Oftentimes pharmaceutical companies will not go after targets that are not expected to be huge blockbusters,” said Waterson, who came to Vanderbilt in 2008 from GlaxoSmithKline where he had worked for seven years on oncology drug development projects. “So an effort like this can fill in a niche that industry is not taking on at the moment.”

One particular area of interest is in screening and developing natural products as potential drug candidates.

This “is something that pharmaceutical industry has de-emphasized just because of the way things have evolved,” said Sulikowski. “And that’s one of our advantages, in that we have expertise in natural products as well as medicinal chemistry.”

Cancer drug development poses many challenges – but also unique opportunities.

“There is a difficulty in that cancer is not a single disease; it’s a family of loosely related diseases,” said Waterson. “There’s an opportunity for a whole myriad of different treatments that are pretty much only tailored to a small subset of people, where your treatment addresses their specific need.”

A unique aspect of the CBC is the NCI’s efforts to establish intellectual property rights for investigators and institutions that develop assays or drug candidates.

“The hope is that by recognizing establishment of intellectual property as one of the goals, they will attract people with the best ideas, things that really might be able to become a drug,” said Waterson.

Vanderbilt’s involvement with the CBC, along with the recent arrival of Stephen Fesik, Ph.D., who previously led cancer drug discovery efforts at Abbott Laboratories, will make Vanderbilt “one of the best academic institutions doing cancer drug discovery in the country,” Marnett said.

Other Vanderbilt investigators involved in this effort include:

• Brian Bachmann, Ph.D., assistant professor of Chemistry and Biochemistry
• Jeffrey Johnston, Ph.D., professor of Chemistry
• Jens Meiler, Ph.D., assistant professor of Chemistry, Pharmacology and Biomedical Informatics
• Craig Lindsley, Ph.D., associate professor of Pharmacology and Chemistry, and director of Medicinal Chemistry

Other sites participating in the CBC are:

• The Burnham Institute for Medical Research, in La Jolla, Calif.;
• Southern Research Institute in Birmingham, Ala.;
• University of North Carolina at Chapel Hill;
• Georgetown University in Washington, D.C.;
• University of Minnesota;
• University of Pittsburgh;
• University of Pittsburgh, Drug Discovery Institute;
• University of California, San Francisco;
• SRI International in Menlo Park, Calif.; and
• Emory University in Atlanta

This project has been funded in whole or in part with Federal Funds from the National Cancer Institute, National Institutes of Health, under Contract No. NO1-CO-12400. The content of this publication does not necessarily reflect the views or policies of the Department of Health and Human Services, nor does mention of trade names, commercial products, or organizations imply endorsement by the U.S. Government.

Source:  vanderbilt.edu