Development of TGF-β signalling inhibitors for cancer therapy
Top Cited Papers
- 1 December 2004
- journal article
- review article
- Published by Springer Nature in Nature Reviews Drug Discovery
- Vol. 3 (12) , 1011-1022
- https://doi.org/10.1038/nrd1580
Abstract
The transforming growth factor-β (TGF-β) 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-β, almost 20 years ago, there have been tremendous advances in our understanding of the complex biology of this superfamily. Deregulation of TGF-β has been implicated in the pathogenesis of a variety of diseases, including cancer and fibrosis. Here we present the rationale for evaluating TGF-β 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.Keywords
This publication has 105 references indexed in Scilit:
- EGFR Mutations in Lung Cancer: Correlation with Clinical Response to Gefitinib TherapyScience, 2004
- Activating Mutations in the Epidermal Growth Factor Receptor Underlying Responsiveness of Non–Small-Cell Lung Cancer to GefitinibNew England Journal of Medicine, 2004
- Smad-dependent and Smad-independent pathways in TGF-β family signallingNature, 2003
- Conditional inactivation of the TGF‐β type II receptor using Cre:LoxGenesis, 2002
- TGF-β signaling: positive and negative effects on tumorigenesisCurrent Opinion in Genetics & Development, 2002
- The TGFβ Receptor Activation ProcessMolecular Cell, 2001
- Molecular mechanisms underlying ErbB2/HER2 action in breast cancerOncogene, 2000
- c-Jun Inhibits Transforming Growth Factor β-mediated Transcription by Repressing Smad3 Transcriptional ActivityPublished by Elsevier ,2000
- New Guidelines to Evaluate the Response to Treatment in Solid TumorsJNCI Journal of the National Cancer Institute, 2000
- Targeted disruption of the mouse transforming growth factor-β1 gene results in multifocal inflammatory diseaseNature, 1992