Document Report Card

ID: ALA1144781

Journal: J Med Chem

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

Authors: Goode DR, Totten RK, Heeres JT, Hergenrother PJ.

Abstract: 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.

CiteXplore: 18366176

DOI: 10.1021/jm701583b