PerspectivePharmacology

Leveraging unique structural characteristics of WNK kinases to achieve therapeutic inhibition

Sci. Signal.  18 Oct 2016:
Vol. 9, Issue 450, pp. pe3
DOI: 10.1126/scisignal.aaj2227

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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 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.

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