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Issue 8, 2015
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Dynamic combinatorial chemistry: a tool to facilitate the identification of inhibitors for protein targets

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Abstract

Dynamic combinatorial chemistry (DCC) has emerged as a powerful strategy to identify ligands for biological targets given that it enables the target to direct the synthesis and amplification of its strongest binder(s) from the library of interconverting compounds. Since the first report of DCC applied to the discovery of binders for a protein, this elegant tool has been employed on a range of protein targets at various stages of medicinal-chemistry projects. A series of suitable, reversible reactions that are biocompatible have been established and the portfolio of analytical techniques is growing. Despite progress, in most cases, the libraries employed remain of moderate size. We present here the most recent advances in the field of DCC applied to protein targets, paying particular attention to the experimental conditions and analytical methods chosen.

Graphical abstract: Dynamic combinatorial chemistry: a tool to facilitate the identification of inhibitors for protein targets

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Publication details

The article was received on 16 Dec 2014 and first published on 23 Feb 2015


Article type: Review Article
DOI: 10.1039/C4CS00493K
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Citation: Chem. Soc. Rev., 2015,44, 2455-2488
  • Open access: Creative Commons BY-NC license
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    Dynamic combinatorial chemistry: a tool to facilitate the identification of inhibitors for protein targets

    M. Mondal and A. K. H. Hirsch, Chem. Soc. Rev., 2015, 44, 2455
    DOI: 10.1039/C4CS00493K

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