| Literature DB >> 30429951 |
Francesca Cantini1,2, Vito Calderone1,2, Lorenzo Di Cesare Mannelli3, Magdalena Korsak2, Leonardo Gonnelli1,2, Oscar Francesconi1, Carla Ghelardini3, Lucia Banci1,2, Cristina Nativi1.
Abstract
The formation of amorphous protein aggregates containing human superoxide dismutase (hSOD1) is thought to be involved in amyotrophic lateral sclerosis onset. cis-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/cis-platin, as hSOD1 antiaggregation lead compound. Oxa/cis-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/cis-platin can be successfully reverted by using lypoyl derivatives, which do not interfere with the antiaggregation properties of the platin derivative.Entities:
Year: 2018 PMID： 30429951 PMCID： PMC6231183 DOI： 10.1021/acsmedchemlett.8b00199
Source DB: PubMed Journal: ACS Med Chem Lett ISSN： 1948-5875 Impact factor: 4.345