8EDH

Identification of a class of WNK isoform-specific inhibitors through high-throughput screening

Summary for 8EDH

• Entry DOI: 10.2210/pdb8edh/pdb
• Descriptor: Serine/threonine-protein kinase WNK3, ethyl 1-(5,7-dimethoxy-4-methylquinolin-2-yl)piperidine-4-carboxylate (3 entities in total)
• Functional Keywords: inhibitor, wnk3, kinase, complex, transferase
• Biological source: Homo sapiens (human)
• Total number of polymer chains: 2
• Total formula weight: 67634.29

Authors

Akella, R.,Goldsmith, E.J. (deposition date: 2022-09-04, release date: 2023-03-01, Last modification date: 2023-10-25)

Primary citation

Chlebowicz, J.,Akella, R.,Humphreys, J.M.,He, H.,Kannangara, A.R.,Wei, S.,Posner, B.,Goldsmith, E.J.
Identification of a Class of WNK Isoform-Specific Inhibitors Through High-Throughput Screening.
Drug Des Devel Ther, 17:93-105, 2023

PubMed Abstract: WNK [with no lysine (K)] kinases are serine/threonine kinases associated with familial hyperkalemic hypertension (FHHt). WNKs are therapeutic targets for blood pressure regulation, stroke and several cancers including triple negative breast cancer and glioblastoma. Here, we searched for and characterized novel WNK kinase inhibitors.

PubMed: 36712947
DOI: 10.2147/DDDT.S389461

Experimental method

X-RAY DIFFRACTION (3.111 Å)