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Novel Approach Assists in Locating Leads for Drug Discovery

Bethesda: The National Institutes of Health (NIH) Chemical Genomics Center, part of the NIH Roadmap for Medical Research's Molecular Libraries and Imaging Initiative,// has reported that a novel method of screening will aid better precision and accuracy in the profiling of compounds in chemical libraries, which will enhance the speed with which data can be utilized to investigate biological procedures, which will support the identification of leads for drug discovery. "We are excited by the power of this approach, developed through the NIH Roadmap for Medical Research, to generate new chemical 'tools' for biological exploration. These tools will help researchers in both the public and private sectors unlock the mysteries of gene function and signaling pathways throughout the human body, opening the door to the development of new drugs," said NIH Director Elias A. Zerhouni, M.D. In a paper published online in the Proceedings of the National Academy of Sciences (PNAS), a team from the NIH Chemical Genomics Center demonstrates the feasibility of a new paradigm for profiling every compound in large collections of chemicals. Traditional high-throughput screening measures the biological activity of chemical compounds at just one concentration. In contrast, the new approach, called quantitative high-throughput screening, or qHTS, tests the biological activity of chemical compounds at seven or more concentration levels spanning four orders of magnitude. The multi-concentration screen produces a pharmacological characterization of all the compounds that is far more complete and reliable than traditional methods. "This advance is crucial to NIH's goal of efficiently profiling the range of biological activities associated with large chemical libraries and making that data swiftly available to the worldwide research community," said Francis S. Collins, M.D., Ph.D., director of the National Human Genome Research Institute (NHGRI). "Broad adoption of this paradigm shou
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