BioCentury | Aug 29, 2017
Distillery Therapeutics

Cardiovascular

...INDICATION: Hypertension In vitro and mouse studies identified an allosteric WNK1 inhibitor that could help treat...
...reported biphenylindole-based allosteric WNK1 inhibitor (IC 50 = 2.14 uM) yielded three compounds that inhibited WNK1...
...testing the compounds and other WNK1 inhibitors in additional models of hypertension. TARGET/MARKER/PATHWAY: WNK lysine deficient protein kinase 1 (WNK1; PPP1R167...
BioCentury | Aug 10, 2017
Preclinical News

Novartis optimizes WNK1 inhibitor hypertension candidate

...of Biomedical Research at Novartis AG (NYSE:NVS; SIX:NOVN) identified an allosteric WNK lysine deficient protein kinase 1 ( WNK1 ; PPP1R167...
...that demonstrated allosteric inhibition via ATP noncompetitive inhibition. Structural analysis led to optimization of a WNK1-specific...
...and core motifs across the scaffolds. In vitro , the compound showed high selectivity for WNK1...
BioCentury | Sep 22, 2016
Distillery Therapeutics

Therapeutics: WNK lysine deficient protein kinase 1 (WNK1; PPP1R167); WNK2; WNK3; WNK4

...and in vitro testing followed by optimization of hits identified an imidazole-oxadiazole-based compound that inhibited WNK1...
...WNK3 and WNK4 activity in vitro with IC50 values below 10 nM and inhibited WNK1...
...could include optimizing and testing the compound in additional models of hypertension. TARGET/MARKER/PATHWAY: WNK lysine deficient protein kinase 1 (WNK1; PPP1R167...
BioCentury | May 19, 2016
Distillery Therapeutics

Therapeutics: MAP kinase 7 (MAPK7; BMK1; ERK-5); mitogen-activated protein kinase kinase kinase 2 (MAP3K2); WNK lysine deficient protein kinase 1 (WNK1; PPP1R16

...mouse and cell culture studies suggest inhibiting MAPK7 or the MAPK7 pathway components MAP3K2 and WNK1...
...normal prostate tissue and high tumor levels of FOXF1 correlated with high tumor levels of WNK1...
...MAPK7; BMK1 ; ERK-5 ); mitogen-activated protein kinase kinase kinase 2 (MAP3K2) ; WNK lysine deficient protein kinase 1 (WNK1; PPP1R167...
BioCentury | Nov 10, 2003
Company News

Lexicon Genetics Inc. other research news

...Researchers published in the Proceedings of the National Academy of Sciences that Wnk1 kinase-deficient mice displayed...
BioCentury | Aug 13, 2001
Company News

Yale University other research news

...Researchers published in Science evidence that mutations of WNK1 and WNK4 serine-threonine kinases play a role...
...a role in the more common essential hypertension. They showed that several mutations of the WNK1...
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