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Vol. 293, Issue 3, 705-709, June 2000

Combinatorial Chemistry and Contemporary Pharmacology

John S. Lazo and Peter Wipf

Departments of Pharmacology and Chemistry, The Fiske Drug Discovery Laboratory and The Combinatorial Chemistry Center, University of Pittsburgh, Pittsburgh, Pennsylvania

Both solid- and liquid-phase combinatorial chemistry have emerged as powerful tools for identifying pharmacologically active compounds and optimizing the biological activity of a lead compound. Complementary high-throughput in vitro assays are essential for compound evaluation. Cell-based assays that use optical endpoints permit investigation of a wide variety of functional properties of these compounds including specific intracellular biochemical pathways, protein-protein interactions, and the subcellular localization of targets. Integration of combinatorial chemistry with contemporary pharmacology now represents an important factor in drug discovery and development.

0022-3565/00/2933-0705$03.00/0
THE JOURNAL OF PHARMACOLOGY AND EXPERIMENTAL THERAPEUTICS
Copyright © 2000 by The American Society for Pharmacology and Experimental Therapeutics


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