Identification of the cellular targets of bioactive small organic molecules using affinity reagents

Benjamin J. Leslie, Paul J. Hergenrother

Research output: Contribution to journalArticle

Abstract

The elucidation of molecular targets of bioactive small organic molecules remains a significant challenge in modern biomedical research and drug discovery. This tutorial review summarizes strategies for the derivatization of bioactive small molecules and their use as affinity probes to identify cellular binding partners. Special emphasis is placed on logistical concerns as well as common problems encountered during such target identification experiments. The roadmap provided is a guide through the process of affinity probe selection, target identification, and downstream target validation.

Original languageEnglish (US)
Pages (from-to)1347-1360
Number of pages14
JournalChemical Society Reviews
Volume37
Issue number7
DOIs
StatePublished - Jun 23 2008

ASJC Scopus subject areas

  • Chemistry(all)

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