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Published October 28, 1997 | Published
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Synthesis and screening of small molecule libraries active in binding to DNA

Shipps, Gerald W., Jr.
Pryor, Kent E.
Xian, Jun
Skyler, David A.
Davidson, Eric H.
Rebek, Julius, Jr.
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Abstract

Five synthetic combinatorial libraries of 2,080 components each were screened as mixtures for inhibition of DNA binding to two transcription factors. Rapid, solution-phase synthesis coupled to a gel-shift assay led to the identification of two compounds active at a 5- to 10-μM concentration level. The likely mode of inhibition is intercalation between DNA base pairs. The efficient deconvolution through sublibrary synthesis augurs well for the use of large mixtures of small, nonpeptide molecules in biological screens.

Additional Information

© 1997 by The National Academy of Sciences. Contributed by Julius Rebek, Jr., August 20, 1997. We thank the Skaggs Foundation for funding and the National Science Foundation for a fellowship to K.E.P. CalTech work was supported by the Beckman Institute of the California Institute of Technology, the National Institutes of Health Grant HD-05753, and by a subcontract from the National Science Foundation Science and Technology Grant BIR9214821. J.X. was supported by National Institutes of Health Training Grant HD-07257. The publication costs of this article were defrayed in part by page charge payment. This article must therefore be hereby marked ''advertisement'' in accordance with 18 U.S.C. §1734 solely to indicate this fact.

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