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

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

Research output: Contribution to journalArticlepeer-review

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.

Original languageEnglish (US)
Pages (from-to)2346-2349
Number of pages4
JournalJournal of Medicinal Chemistry
Volume51
Issue number8
DOIs
StatePublished - Apr 24 2008

ASJC Scopus subject areas

  • Molecular Medicine
  • Drug Discovery

Fingerprint Dive into the research topics of 'Identification of promiscuous small molecule activators in high-throughput enzyme activation screens'. Together they form a unique fingerprint.

Cite this