Yamada, Ken, Park, Hyi-Man, Rigel, Dean, Monovich, Lauren, Whalen, Erin, Anisowicz, Anthony, Beil, Michael, Berstler, James, Brocklehurst, Cara, Burdick, Debra, Caplan, Shari, Capparelli, Michael, Chen, Guanjing, Chen, Wei, Dale, Bethany, Deng, Lin, Fu, Fumin, Hamamatsu, Norio, Harasaki, Kouki, Herr, Tracey, Hoffmann, Peter, Hu, Qi-Ying, Huang, Waanjeng, Idamakanti, Neeraja, Imase, Hidetomo, Iwaki, Yuki, Jain, Monish, Jeyaseelan, Jey, Kato, Mitsunori, Kaushik, Virendar, Kohls, Darcy, Kunjathoor, Vidya, Lasala, Daniel, Lee, Jongchan, Liu, Jing, Luo, Yang, Ma, Fupeng, Mo, Ruowei, Mowbray, Sarah, Mogi, Muneto, Ossola, Flavio, Pandey, Pramod, Patel, Sejal, Raghavan, Swetha, Salem, Bahaa, Shanado, Yuka, Trakshel, Gary, Turner, Gordon, Wakai, Hiromichi, Wang, Chunhua, Weldon, Stephen, Wielicki, Jennifer, Xie, Xiaoling, Xu, Lingfei, Yagi, Yukiko, Yasoshima, Kayo, Yin, Jianning, Yowe, David, Zhang, Ji, Zheng, Gang and Dipetrillo, Keith (2016) Small-molecule WNK inhibition regulates cardiovascular and renal function. Nature Chemical Biology, 12 (11). pp. 896-898. ISSN 15524469

Abstract

The With-No-Lysine (K) (WNK) kinases play a critical role in blood pressure regulation and body fluid and electrolyte homeostasis. Herein, we introduce the first orally bioavailable pan-WNK-kinase inhibitor, WNK463, that exploits unique structural features of the WNK kinases for both affinity and kinase selectivity. In rodent models of hypertension, WNK463 affects blood pressure and body fluid and electro-lyte homeostasis, consistent with WNK-kinase-associated physiology and pathophysiology.

Item Type:	Article
Date Deposited:	26 Oct 2024 00:46
Last Modified:	26 Oct 2024 00:46
URI:	https://oak.novartis.com/id/eprint/24957