| Literature DB >> 27595330 |
Ken Yamada1, Hyi-Man Park1, Dean F Rigel1, Keith DiPetrillo1, Erin J Whalen1, Anthony Anisowicz1, Michael Beil1, James Berstler1, Cara Emily Brocklehurst1, Debra A Burdick1, Shari L Caplan1, Michael P Capparelli1, Guanjing Chen1, Wei Chen1, Bethany Dale1, Lin Deng1, Fumin Fu1, Norio Hamamatsu1, Kouki Harasaki1, Tracey Herr1, Peter Hoffmann1, Qi-Ying Hu1, Waan-Jeng Huang1, Neeraja Idamakanti1, Hidetomo Imase1, Yuki Iwaki1, Monish Jain1, Jey Jeyaseelan1, Mitsunori Kato1, Virendar K Kaushik1, Darcy Kohls1, Vidya Kunjathoor1, Daniel LaSala1, Jongchan Lee1, Jing Liu1, Yang Luo1, Fupeng Ma1, Ruowei Mo1, Sarah Mowbray1, Muneto Mogi1, Flavio Ossola1, Pramod Pandey1, Sejal J Patel1, Swetha Raghavan1, Bahaa Salem1, Yuka H Shanado1, Gary M Trakshel1, Gordon Turner1, Hiromichi Wakai1, Chunhua Wang1, Stephen Weldon1, Jennifer B Wielicki1, Xiaoling Xie1, Lingfei Xu1, Yukiko I Yagi1, Kayo Yasoshima1, Jianning Yin1, David Yowe1, Ji-Hu Zhang1, Gang Zheng1, Lauren Monovich1.
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.Entities:
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Year: 2016 PMID： 27595330 DOI： 10.1038/nchembio.2168
Source DB: PubMed Journal: Nat Chem Biol ISSN： 1552-4450 Impact factor: 15.040