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Nat Chem Biol. 2016 Nov;12(11):896-898. doi: 10.1038/nchembio.2168. Epub 2016 Sep 5.

Small-molecule WNK inhibition regulates cardiovascular and renal function.

Author information

1
Novartis Institutes for BioMedical Research, Cambridge, Massachusetts, USA.

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.

PMID:
27595330
DOI:
10.1038/nchembio.2168
[Indexed for MEDLINE]

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