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Future Med Chem. 2015;7(2):159-83. doi: 10.4155/fmc.14.152.

Photoaffinity labeling in target- and binding-site identification.

Author information

1
Cancer Research UK Cancer Therapeutics Unit, The Institute of Cancer Research, 15 Cotswold Road, Sutton, Surrey, SM2 5NG, London, UK.

Abstract

Photoaffinity labeling (PAL) using a chemical probe to covalently bind its target in response to activation by light has become a frequently used tool in drug discovery for identifying new drug targets and molecular interactions, and for probing the location and structure of binding sites. Methods to identify the specific target proteins of hit molecules from phenotypic screens are highly valuable in early drug discovery. In this review, we summarize the principles of PAL including probe design and experimental techniques for in vitro and live cell investigations. We emphasize the need to optimize and validate probes and highlight examples of the successful application of PAL across multiple disease areas.

PMID:
25686004
PMCID:
PMC4413435
DOI:
10.4155/fmc.14.152
[Indexed for MEDLINE]
Free PMC Article

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