Target identification of bioactive compounds

Bioorg Med Chem. 2012 Mar 15;20(6):1910-21. doi: 10.1016/j.bmc.2011.10.081. Epub 2011 Nov 4.

Abstract

To fully understand the regulation of cellular events, functional analysis of each protein involved in the regulatory systems is required. Among a variety of methods to uncover protein function, chemical genetics is a remarkable approach in which small molecular compounds are used as probes to elucidate protein functions within signaling pathways. However, identifying the target of small molecular bioactive compounds isolated by cell-based assays represents a crucial hurdle that must be overcome before chemical genetic studies can commence. A variety of methods and technologies for identifying target proteins have been reported. This review therefore aims to describe approaches for identifying these molecular targets.

Publication types

  • Review

MeSH terms

  • Animals
  • Computational Biology / methods*
  • Drug Discovery / methods*
  • Humans
  • Proteins / metabolism*
  • Signal Transduction / drug effects
  • Small Molecule Libraries / chemistry
  • Small Molecule Libraries / pharmacology*

Substances

  • Proteins
  • Small Molecule Libraries