Issue 7, 2008
From the journal:

Chemical Society Reviews

Small-molecule microarrays as tools in ligand discovery†

Arturo J. Vegas,a   Jason H. Fullerb  and  Angela N. Koehler*b  

* Corresponding authors

a Department of Chemical Engineering, Massachusetts Institute of Technology, Cambridge, Massachusetts, USA

b Broad Institute of Harvard and MIT, Cambridge, Massachusetts, USA
E-mail: koehler@fas.harvard.edu
Fax: +1-617-324-9601
Tel: +1-617-324-9634

Abstract

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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Article information

DOI
https://doi.org/10.1039/B703568N
Article type
Tutorial Review
Submitted
21 Apr 2008
First published
20 May 2008

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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