8EDH

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

8EDH の概要

• エントリーDOI: 10.2210/pdb8edh/pdb
• 分子名称: Serine/threonine-protein kinase WNK3, ethyl 1-(5,7-dimethoxy-4-methylquinolin-2-yl)piperidine-4-carboxylate (3 entities in total)
• 機能のキーワード: inhibitor, wnk3, kinase, complex, transferase
• 由来する生物種: Homo sapiens (human)
• タンパク質・核酸の鎖数: 2
• 化学式量合計: 67634.29

構造登録者

Akella, R.,Goldsmith, E.J. (登録日: 2022-09-04, 公開日: 2023-03-01, 最終更新日: 2023-10-25)

主引用文献

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

実験手法

X-RAY DIFFRACTION (3.111 Å)