학술논문
Kinetic characterization of novel pyrazole TGF-beta receptor I kinase inhibitors and their blockade of the epithelial-mesenchymal transition
Document Type
Academic Journal
Author
Source
Biochemistry. Feb 22, 2005, Vol. 44 Issue 7, p2293, 12 p.
Subject
Language
English
ISSN
0006-2960
Abstract
A short phospho-Smad peptide, pSmad3(--3), KVLTQMGSPSIRCSS(PO4)VS as a substrate of transforming growth factor beta (TGF-beta) type-I receptor (TbetaRI) kinase for in vitro kinase assays is identified. The functional analysis revealed that pyrazoles are capable of blocking the TGF-beta-induced epithelial--mesenchymal transition in NMuMg cells, a process involved in the progression of cancer, fibrosis and other human diseases.