Issue 3, 2014

Affinity-based target identification for bioactive small molecules

Abstract

Identification of the cellular targets of bioactive small molecules is a crucial step in drug discovery and chemical genetics. Classical affinity purification with small-molecule affinity probes remains the most common approach, but it remains a considerable challenge. To overcome various drawbacks in probe preparation, nonspecific interactions, and the sensitivity of target detection, new methods and techniques are being developed, such as a nonselective universal coupling method based on a photo-affinity reaction, which enables introduction of a variety of small molecules to a solid support without chemical modification to generate small-molecule affinity probes. Here, we review recent progress in affinity-based approaches for small-molecule target identification with a focus on affinity purification.

Graphical abstract: Affinity-based target identification for bioactive small molecules

Article information

Article type
Review Article
Submitted
25 Sep 2013
Accepted
02 Dec 2013
First published
04 Dec 2013

Med. Chem. Commun., 2014,5, 277-287

Affinity-based target identification for bioactive small molecules

M. Kawatani and H. Osada, Med. Chem. Commun., 2014, 5, 277 DOI: 10.1039/C3MD00276D

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