Identification of promiscuous small molecule activators in high-throughput enzyme activation screens.

David R Goode, Ryan K Totten, James T Heeres, Paul J Hergenrother

Department of Chemistry, Roger Adams Laboratory, University of Illinois, 600 S. Mathews Avenue, Urbana, Illinois 61801, USA.

Journal of medicinal chemistry 2008 Apr 24

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It is recognized that high-throughput enzyme inhibition screens often return nonspecific inhibitors as "hits". Recently, high-throughput screens for enzyme activators have led to the identification of several compounds with novel and potent biological activity. Here, we show that enzyme activation screens can also uncover compounds that activate multiple enzymes in a nonspecific fashion. Described herein are the general structural features of such compounds and methods to differentiate between specific and general enzyme activation.

Citation

David R Goode, Ryan K Totten, James T Heeres, Paul J Hergenrother. Identification of promiscuous small molecule activators in high-throughput enzyme activation screens. Journal of medicinal chemistry. 2008 Apr 24;51(8):2346-9