Home
Resources
Publications
Identification of Ebselen as a Potent Inhibitor of Insulin Degrading Enzyme by a Drug Repurposing Screening

Identification of Ebselen as a Potent Inhibitor of Insulin Degrading Enzyme by a Drug Repurposing Screening

Florence Leroux, Damien Bosc, Terence Beghyn, Paul Hermant, Sandrine Warenghem, Valérie Landry, Virginie Pottiez, Valentin Guillaume, Julie Charton, Adrien Herledan, Sarah Urata, Wenguang Liang, Li Sheng, etc.

Eur J Med Chem. 2019 Oct 1;179:557-566.

PMID: 31276900

Abstract:

Insulin-degrading enzyme, IDE, is a metalloprotease implicated in the metabolism of key peptides such as insulin, glucagon, β-amyloid peptide. Recent studies have pointed out its broader role in the cell physiology. In order to identify new drug-like inhibitors of IDE with optimal pharmacokinetic properties to probe its multiple roles, we ran a high-throughput drug repurposing screening. Ebselen, cefmetazole and rabeprazole were identified as reversible inhibitors of IDE. Ebselen is the most potent inhibitor (IC50(insulin) = 14 nM). The molecular mode of action of ebselen was investigated by biophysical methods. We show that ebselen induces the disorder of the IDE catalytic cleft, which significantly differs from the previously reported IDE inhibitors. IDE inhibition by ebselen can explain some of its reported activities in metabolism as well as in neuroprotection.

Chemicals Related in the Paper:

Catalog Number	Product Name	Structure	CAS Number	Price
AP60940343	Ebselen		60940-34-3	Price

As a specialist in analytical chemical Products, Alfa Chemistry offers consumers a wealth of raw materials and a full range of technologies and services.

QUICK LINKS

HEADQUARTERS

Tel:

Fax:

Email: