Description
GW-788388 inhibits activin receptor-like kinase 5 (ALK5), suppressing TGF-β activity; it exhibits anti-fibrotic and cardioprotective activities. GW-788388 increases survival in studies of Trypanosoma infection and prevents Chagas disease-induced development of cardiac fibrosis. This compound also attenuates systolic dysfunction and left ventricular remodeling in animal models of myocardial infarction. In animal models of diabetes, GW-788388 decreases the occurrence of renal fibrosis.
References
de Oliveira FL, Araújo-Jorge TC, de Souza EM, et al. Oral administration of GW788388, an inhibitor of transforming growth factor beta signaling, prevents heart fibrosis in Chagas disease. PLoS Negl Trop Dis. 2012;6(6):e1696. PMID: 22720109.
Tan SM, Zhang Y, Connelly KA, et al. Targeted inhibition of activin receptor-like kinase 5 signaling attenuates cardiac dysfunction following myocardial infarction. Am J Physiol Heart Circ Physiol. 2010 May;298(5):H1415-25. PMID: 20154262.
Petersen M, Thorikay M, Deckers M, et al. Oral administration of GW788388, an inhibitor of TGF-beta type I and II receptor kinases, decreases renal fibrosis. Kidney Int. 2008 Mar;73(6):705-15. PMID: 18075500.
