Work

Leveraging unique structural characteristics of WNK kinases to achieve therapeutic inhibition

Year: 2016

Type: article

Abstract: 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.

Source: Science Signaling

DOI: 10.1126/scisignal.aaj2227

Authors: Jinwei Zhang, Xianming Deng, Kristopher T. Kahle

Institutions: University of Dundee, MRC Protein Phosphorylation and Ubiquitylation Unit, Xiamen University, Yale University

Language: English

Topic: Ion Transport and Channel Regulation

Subfield: Molecular Biology

Field: Biochemistry, Genetics and Molecular Biology

Domain: Life Sciences

SDG: Good health and well-being

Open Access status: green

OpenAlex ID: W2536633292