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Issue 3, 2014
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Affinity-based target identification for bioactive small molecules

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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

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Publication details

The article was received on 25 Sep 2013, accepted on 02 Dec 2013 and first published on 04 Dec 2013

Article type: Review Article
DOI: 10.1039/C3MD00276D
Citation: Med. Chem. Commun., 2014,5, 277-287

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    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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