Small-molecule WNK inhibition regulates cardiovascular and renal function
K Yamada, HM Park, DF Rigel, K DiPetrillo… - Nature chemical …, 2016 - nature.com
K Yamada, HM Park, DF Rigel, K DiPetrillo, EJ Whalen, A Anisowicz, M Beil, J Berstler…
Nature chemical biology, 2016•nature.comAbstract 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.
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.
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.
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