Development of TGF-beta signalling inhibitors for cancer therapy

Nat Rev Drug Discov. 2004 Dec;3(12):1011-22. doi: 10.1038/nrd1580.


The transforming growth factor-beta (TGF-beta) superfamily of ligands has a pivotal role in the regulation of a wide variety of physiological processes from development to pathogenesis. Since the discovery of the prototypic member, TGF-beta, almost 20 years ago, there have been tremendous advances in our understanding of the complex biology of this superfamily. Deregulation of TGF-beta has been implicated in the pathogenesis of a variety of diseases, including cancer and fibrosis. Here we present the rationale for evaluating TGF-beta signalling inhibitors as cancer therapeutics, the structures of small-molecule inhibitors that are in development and the targeted drug discovery model that is being applied to their development.

Publication types

  • Review

MeSH terms

  • Animals
  • Antineoplastic Agents / chemistry
  • Antineoplastic Agents / pharmacology
  • Antineoplastic Agents / therapeutic use*
  • Drug Design
  • Humans
  • Neoplasms / drug therapy*
  • Neoplasms / metabolism
  • Signal Transduction / drug effects*
  • Signal Transduction / physiology
  • Transforming Growth Factor beta / antagonists & inhibitors*
  • Transforming Growth Factor beta / metabolism


  • Antineoplastic Agents
  • Transforming Growth Factor beta