Emerging classes of protein-protein interaction inhibitors and new tools for their development

Curr Opin Chem Biol. 2004 Aug;8(4):442-9. doi: 10.1016/j.cbpa.2004.06.006.


Protein-protein interactions play a key role in the signal transduction pathways that regulate cellular function. Three years ago, few descriptions of small molecule protein-protein interaction inhibitors (SMPPIIs) existed in the literature. Today, the number of examples of both the biology and chemistry of such interaction inhibitors is growing rapidly. This growth occurs at the convergence of medicinal chemistry, signaling biology and novel assay technology for profiling emerging compound classes and modes of action. Protein translocation assays provide a unique new tool for identifying, profiling, and optimizing SMPPIIs. This review summarizes recent work in the field, and outlines future developments we can anticipate.

Publication types

  • Review

MeSH terms

  • Animals
  • Computational Biology
  • Drug Design*
  • Humans
  • Models, Biological
  • Models, Molecular
  • Molecular Structure
  • Protein Binding / drug effects
  • Proteins / antagonists & inhibitors*
  • Proteins / metabolism*
  • Signal Transduction / drug effects
  • Signal Transduction / physiology


  • Proteins