In vivo selective inhibition of TRPC6 by antagonist BI 749327 ameliorates fibrosis and dysfunction in cardiac and renal disease [Physiology]

Transient receptor potential canonical type 6 (TRPC6) is a nonselective receptor-operated cation channel that regulates reactive fibrosis and growth signaling. Increased TRPC6 activity from enhanced gene expression or gain-of-function mutations contribute to cardiac and/or renal disease. Despite evidence supporting a pathophysiological role, no orally bioavailable selective TRPC6 inhibitor has yet...

Source: Proceedings of the National Academy of Sciences - May 13, 2019 Category: Science Authors: Brian Leei Lin, Damian Matera, Julia F. Doerner, Nan Zheng, Donato del Camino, Sumita Mishra, Hong Bian, Svetlana Zeveleva, Xiaoguang Zhen, Nathaniel T. Blair, Jayhong A. Chong, David P. Hessler, Djahida Bedja, Guangshuo Zhu, Grace K. Muller, Mark J. Rane Tags: Biological Sciences Source Type: research