SAN DIEGO, Nov. 6 /PRNewswire/ -- The Genomics Institute of the Novartis Research Foundation (GNF) and ChemBridge Research Laboratories, LLC (CRL) announced results on GNF's evaluation of CRL's GPCR Targeted Library. Key advantages were discovered during the investigation of CRL's compounds against a number of undisclosed Class A, B and C, G-protein coupled receptor (GPCRs) targets. Advantages include both the identification of confirmed active hits of highest potency in all of the GPCR targets screened including the highest hit rate against the least tractable target and the characterization of CRL compounds by GNF medicinal chemists as the most "chemically attractive" for further lead optimization due to the appearance of a defined structural activity relationship. GNF and CRL in December 2002 entered into the agreement that provided, among other undisclosed terms, access for GNF and its affiliates, including Novartis AG, to CRL's GPCR Targeted Library.
CRL's de-novo approach involves the design and synthesis of library templates that mimic selected secondary structures of conserved regions of endogenous ligands applicable for various GPCR sub-families. Such information, unified with careful in silico profiled lead-like molecular properties and an innovative as well systematic chemistry effort produces novel highly pure compounds of desirable structural diversity. Currently more than 70% of the drugs on the market are targeted to GPCRs and challenging GPCR targets are expected to continue to be key in the search for effective drugs across many therapeutic indications.
"We are very pleased with the quality of the CRL GPCR-focused library," said Jeremy Caldwell, Ph.D., GNF's Director of Molecular and Cellular Biology, "particularly since the library helped us to resurrect several projects that we had previously dropped due to lack of leads."
Sven H. Wagner, Ph.D., Associate Director of Business Development of CRL, said: "GNF is well known for its excellence in developing advanced screening technologies and applying such in lead discovery. Our GPCR Targeted Library represents a useful tool to enable further dynamic optimization efforts for the discovery of a range of receptors that are currently without effective drug candidates. The progress exemplified by GNF's benchmark study is encouraging and we look forward to share with other partners in highly targeted applications the utility of our medicinal chemistry expertise in this rich target class."
ChemBridge Research Laboratories, LLC (CRL), http://www.chembridgeresearch.com/ , is a discovery chemistry research company based in San Diego. CRL's state-of- the-art custom built laboratories encompass high-throughput, medicinal, large scale, analytical, and computational chemistry capabilities. CRL can tackle the most challenging discovery chemistry projects by leveraging its access to a portfolio of unique chemistry tools and knowledge database of validated synthetic methodologies applicable to drug discovery. CRL's growth in the near and long-term will be supported by a balanced portfolio of proprietary products, such as advanced combinatorial libraries against GPCR, Kinases and several other important protein super-families, multiple discovery/medicinal chemistry contract research arrangements with pharmaceutical and leading biotech companies, as well as proprietary lead identification programs.
About the Genomics Institute of the Novartis Research Foundation (GNF)
Founded in 1999, the Genomics Institute of the Novartis Research Foundation (GNF) houses over 200 scientists and engineers who are revolutionizing experimental science in the postgenomic era. The Institute is funded through the Novartis Research Foundation as a research center in which scientists have freedom to conduct independent research. Scientists at GNF pursue groundbreaking research and publish papers that represent fundamental advances in their fields. The Institute is developing advanced technologies ranging from cellular genomics and proteomics to combinatorial chemistry and structural biology. The spectrum of technologies developed at GNF enables scientists to study thousands of genes/proteins each day, accelerating the discovery process and dramatically enhancing the insights that can be obtained. In addition to technology development and basic biomedical research, GNF is focused on developing treatments for a host of human disorders, including neurodegenerative and metabolic diseases and cancer. GNF maintains a close relationship with Novartis AG and other Novartis entities, engaging in collaborative projects to expand technological innovation and accelerate the drug discovery process. Collaborations with academic groups and biotech firms are also strongly encouraged. In addition to its unparalleled internal resources, GNF is located in close proximity to the Scripps Research Institute, the Salk Institute, the Burnham Institute and the University of California, San Diego.
ChemBridge Research Laboratories, LLC (CRL)