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Issue 7, 2008
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Identification of the cellular targets of bioactive small organic molecules using affinity reagents

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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.

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

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Article information


Submitted
11 Apr 2008
First published
23 May 2008

Chem. Soc. Rev., 2008,37, 1347-1360
Article type
Tutorial Review

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

B. J. Leslie and P. J. Hergenrother, Chem. Soc. Rev., 2008, 37, 1347
DOI: 10.1039/B702942J

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