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Issue 7, 2008
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Small-molecule microarrays as tools in ligand discovery

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Small molecules that bind and modulate specific protein targets are increasingly used as tools to decipher protein function in a cellular context. Identifying specific small-molecule probes for each protein in the proteome will require miniaturized assays that permit screening of large collections of compounds against large numbers of proteins in a highly parallel fashion. Simple and general binding assays involving small-molecule microarrays can be used to identify probes for nearly any protein in the proteome. The assay may be used to identify ligands for proteins in the absence of knowledge about structure or function. In this tutorial review, we introduce small-molecule microarrays (SMMs) as tools for ligand discovery; discuss methods for manufacturing SMMs, including both non-covalent and covalent attachment strategies; and provide examples of ligand discovery involving SMMs.

Graphical abstract: Small-molecule microarrays as tools in ligand discovery

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Publication details

The article was received on 21 Apr 2008 and first published on 20 May 2008

Article type: Tutorial Review
DOI: 10.1039/B703568N
Chem. Soc. Rev., 2008,37, 1385-1394

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    Small-molecule microarrays as tools in ligand discovery

    A. J. Vegas, J. H. Fuller and A. N. Koehler, Chem. Soc. Rev., 2008, 37, 1385
    DOI: 10.1039/B703568N

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