6FFK

Human apo-SOD1 bound to PtCl2(1R,2R-1,4-DACH

6FFK の概要

• エントリーDOI: 10.2210/pdb6ffk/pdb
• 関連するPDBエントリー: 3re0
• 分子名称: Superoxide dismutase [Cu-Zn], PtCl2(1(R),2(R)-DACH) (3 entities in total)
• 機能のキーワード: oxidoreductase
• 由来する生物種: Homo sapiens (human)
• タンパク質・核酸の鎖数: 4
• 化学式量合計: 64822.87

構造登録者

Calderone, V.,Nativi, C.,Cantini, F.,Di Cesare Mannelli, L. (登録日: 2018-01-08, 公開日: 2018-11-28, 最終更新日: 2024-10-16)

主引用文献

Cantini, F.,Calderone, V.,Di Cesare Mannelli, L.,Korsak, M.,Gonnelli, L.,Francesconi, O.,Ghelardini, C.,Banci, L.,Nativi, C.
Interaction of Half Oxa-/Halfcis-Platin Complex with Human Superoxide Dismutase and Induced Reduction of Neurotoxicity.
ACS Med Chem Lett, 9:1094-1098, 2018

PubMed Abstract: The formation of amorphous protein aggregates containing human superoxide dismutase (hSOD1) is thought to be involved in amyotrophic lateral sclerosis onset. -Platin inhibits the oligomerization of apo hSOD1, but its toxicity precludes any possible use in therapy. Herein, we propose a less toxic platinum complex, namely oxa/-platin, as hSOD1 antiaggregation lead compound. Oxa/-platin is able to interact with hSOD1 in the disulfide oxidized apo form by binding cysteine 111 (Cys111). The mild neurotoxic phenomena induced in vitro and in vivo by oxa/-platin can be successfully reverted by using lypoyl derivatives, which do not interfere with the antiaggregation properties of the platin derivative.

PubMed: 30429951
DOI: 10.1021/acsmedchemlett.8b00199

実験手法

X-RAY DIFFRACTION (1.94 Å)