Identification of direct protein targets of small molecules

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

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.

Publication types

  • Research Support, N.I.H., Extramural
  • Research Support, Non-U.S. Gov't
  • Review

MeSH terms

  • Chromatography, Affinity
  • Drug Delivery Systems
  • Drug Design*
  • Molecular Targeted Therapy / methods*
  • Pharmaceutical Preparations
  • Protein Binding / physiology*
  • Proteome / chemistry*
  • Proteomics
  • Small Molecule Libraries / chemistry*

Substances

  • Pharmaceutical Preparations
  • Proteome
  • Small Molecule Libraries