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ACS Chem Biol. 2011 Jan 21;6(1):34-46. doi: 10.1021/cb100294v. Epub 2010 Nov 30.

Identification of direct protein targets of small molecules.

Author information

1
Department of Molecular and Medical Pharmacology, University of California, Los Angeles, 90095, United States.

Abstract

Small-molecule target identification is a vital and daunting task for the chemical biology community as well as for researchers interested in applying the power of chemical genetics to impact biology and medicine. To overcome this "target ID" bottleneck, new technologies are being developed that analyze protein-drug interactions, such as drug affinity responsive target stability (DARTS), which aims to discover the direct binding targets (and off targets) of small molecules on a proteome scale without requiring chemical modification of the compound. Here, we review the DARTS method, discuss why it works, and provide new perspectives for future development in this area.

PMID:
21077692
PMCID:
PMC3031183
DOI:
10.1021/cb100294v
[Indexed for MEDLINE]
Free PMC Article

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