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

Development of TGF-beta signalling inhibitors for cancer therapy.

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Lilly Research Laboratories, Eli Lilly and Company, Indianapolis, Indiana 46285, USA.


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.

[Indexed for MEDLINE]

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