Discovery Series

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Molecular Targeted Assays

A variety of molecular targeted drug screening assays have been developed by the Developmental Therapeutics Program in collaboration with various investigators. A number of additional assay are currently under development. These vary in format, ranging from simple cell-free assays to those involving cell lines engineered to express particular reporter systems. The screening assays are intended for use in conjunction with chemical libraries to support discovery of novel molecular targeted agents, or drug leads, relevant to treatment of cancer, AIDS-associated malignancies, HIV-1 disease or opportunistic infections. For a recent review of the process, see Shoemaker, et al. Application of High-Throughput, Molecular-Targeted Screening to Anticancer Drug Discovery. Current Topics in Medicinal Chemistry 2:229-246, 2002. A downloadable copy of this review is available at: http://spheroid.ncifcrf.gov/stb/staff/shoemaker/ShoemakerR_CurrTopMedChem2002p229.pdf. Data generated during assay development (screening data on the NCI Training Set) and results from high-throughput screening of the NCI Diversity Set are available on this page.

The Diversity Set has been utilized by a variety of extramural research groups for molecular-targeted screening. For example, Lazo et al. have identified Cdc25 phosphatase inhibitors (Mol Pharmacol 61:720-728, 2002); Bykov et al. identified a compound which restores function in p53 mutant tumor cells and demonstrates in vivo antitumor activity (Nature Medicine 8:282-288, 2002); and Kao et al. have identified inhibitors of angiogenin (Proc Natl Acad Sci U S A 2002 Jul 12; [epub ahead of print]).

Click here to download text data files for each of the molecularly targeted drug screening assays.