Leveraging unique structural characteristics of WNK kinases to achieve therapeutic inhibition
Zhang, J; Deng, X; Kahle, KT
Date: 18 October 2016
Journal
Science Signaling
Publisher
American Association for the Advancement of Science
Publisher DOI
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Abstract
The with-no-lysine (K) WNK kinases are master regulators of the Na+-(K+)-Cl- cotransporters, including the renal-specific NCC and NKCC2 cotransporters. The discovery of WNK463, an orally bioavailable pan-WNK kinase inhibitor that exploits unique structural properties of the WNK catalytic domain to achieve high affinity and kinase ...
The with-no-lysine (K) WNK kinases are master regulators of the Na+-(K+)-Cl- cotransporters, including the renal-specific NCC and NKCC2 cotransporters. The discovery of WNK463, an orally bioavailable pan-WNK kinase inhibitor that exploits unique structural properties of the WNK catalytic domain to achieve high affinity and kinase selectivity, illustrates a strategy of leveraging distinct kinase features to develop specific inhibitors and validates the genetic predictions of the in vivo pharmacology of WNK inhibition.
Institute of Biomedical & Clinical Science
Collections of Former Colleges
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