Article
Structural basis for specificity of TGFβ family receptor small molecule inhibitors.
Cellular signalling - 1 Feb 2012
Ogunjimi Abiodun A, Zeqiraj Elton, Ceccarelli Derek F, Sicheri Frank, Wrana Jeffrey L, David Laurent
Abstract excerpt
Transforming growth factor-β (TGFβ) receptor kinase inhibitors have a great therapeutic potential. SB431542 is one of the mainly used kinase inhibitors of the TGFβ/Activin pathway receptors, but needs improvement of its EC(50) (EC(50)=1 μM) to be translated to clinical use. A key feature of SB431542 is that it specifically targets receptors from the TGFβ/Activin pathway but not the closely related receptors from...
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