Recent advances and method development for drug target identification

Trends Pharmacol Sci. 2010 Feb;31(2):82-8. doi: 10.1016/ Epub 2009 Dec 7.


Although it is commonly recognized that most drugs cause inhibition or activation of function by physically binding to one or more gene products, the direct interactions of bioactive small molecules with specific gene products, or targets, is often not well characterized. From a therapeutic perspective, it is nevertheless essential to know a drug's binding partner(s) to understand the mechanism of action and anticipate possible side effects to avoid costly clinical failures. This knowledge is increasingly important as the prevalence of polypharmacy expands to include drugs that engage multiple targets. This review provides a succinct overview of several recent approaches that employ genetics, proteomics, expression profiling or bioinformatics procedures for the systematic characterization of the targets of bioactive compounds. The continuous improvement and advancement of existing technologies is critically discussed and we offer a perspective on the future of innovative emerging new generation technologies.

Publication types

  • Research Support, Non-U.S. Gov't
  • Review

MeSH terms

  • Computational Biology
  • Drug Discovery*
  • Drug Evaluation, Preclinical
  • Gene Expression Profiling
  • High-Throughput Screening Assays
  • Proteomics