8A46

Crystal structure of the human Kelch domain of Keap1 in complex with compound S217879

8A46 の概要

• エントリーDOI: 10.2210/pdb8a46/pdb
• 分子名称: Kelch-like ECH-associated protein 1, 2-[(1S,2R,8S)-2,4,32-trimethyl-28,28-bis(oxidanylidene)-19,22,27-trioxa-28$l^{6}-thia-1,14,15,16-tetrazahexacyclo[21.5.3.1^{3,7}.1^{9,13}.0^{12,16}.0^{26,30}]tritriaconta-3(33),4,6,9(32),10,12,14,23,25,30-decaen-8-yl]ethanoic acid (3 entities in total)
• 機能のキーワード: master regulator of cellular resistance to oxidants, transcription
• 由来する生物種: Mus musculus (house mouse)
• タンパク質・核酸の鎖数: 1
• 化学式量合計: 34368.43

構造登録者

Weber, C.,Vuillard, L.,Delerive, P.,Miallau, L. (登録日: 2022-06-10, 公開日: 2022-07-13, 最終更新日: 2024-05-01)

主引用文献

Seedorf, K.,Weber, C.,Vinson, C.,Berger, S.,Vuillard, L.M.,Kiss, A.,Creusot, S.,Broux, O.,Geant, A.,Ilic, C.,Lemaitre, K.,Richard, J.,Hammoutene, A.,Mahieux, J.,Martiny, V.,Durand, D.,Melchiore, F.,Nyerges, M.,Paradis, V.,Provost, N.,Duvivier, V.,Delerive, P.
Selective disruption of NRF2-KEAP1 interaction leads to NASH resolution and reduction of liver fibrosis in mice.
JHEP Rep, 5:100651-100651, 2023

PubMed Abstract: Oxidative stress is recognized as a major driver of non-alcoholic steatohepatitis (NASH) progression. The transcription factor NRF2 and its negative regulator KEAP1 are master regulators of redox, metabolic and protein homeostasis, as well as detoxification, and thus appear to be attractive targets for the treatment of NASH.

PubMed: 36866391
DOI: 10.1016/j.jhepr.2022.100651

実験手法

X-RAY DIFFRACTION (1.323 Å)