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Chem Soc Rev DOI:10.1039/b703568n

Small-molecule microarrays as tools in ligand discovery.

Publication TypeJournal Article
Year of Publication2008
AuthorsVegas, AJ, Fuller, JH, Koehler, AN
JournalChem Soc Rev
Date Published2008 Jul
KeywordsBinding Sites, Biological Assay, Ligands, Microarray Analysis, Proteins, Small Molecule Libraries

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.


Alternate JournalChem Soc Rev
PubMed ID18568164
PubMed Central IDPMC2688956
Grant ListN01 CO012400 / CO / NCI NIH HHS / United States
N01CO12400 / CA / NCI NIH HHS / United States
N01-CO-12400 / CO / NCI NIH HHS / United States