Small Changes Make the Difference for SIRT2: Two Different Binding Modes for 3-Arylmercapto-Acylated Lysine Derivatives

Autor:	Diana Kalbas, Marat Meleshin, Sandra Liebscher, Matthes Zessin, Jelena Melesina, Cordelia Schiene-Fischer, Emre Fatih Bülbül, Frank Bordusa, Wolfgang Sippl, Mike Schutkowski
Rok vydání:	2022
Předmět:	Niacinamide Sirtuin 2 Catalytic Domain Lysine Humans Sirtuins Peptides Biochemistry
Zdroj:	Biochemistry. 61:1705-1722
ISSN:	1520-4995 0006-2960
DOI:	10.1021/acs.biochem.2c00211
Popis:	Sirtuins are protein deacylases regulating metabolism and stress responses and implicated in aging-related diseases. Modulators of the human sirtuins 1-7 are sought as chemical tools and potential therapeutics, for example, for treatment of cancer. We were able to show that 3-aryl-mercapto-succinylated- and 3-benzyl-mercapto-succinylated peptide derivatives yield selective Sirt5 inhibitors with low nM
Databáze:	OpenAIRE
Externí odkaz:	https://explore.openaire.eu/search/publication?articleId=doi_dedup___::7ff127a0bbd786175cd40279267377bf https://doi.org/10.1021/acs.biochem.2c00211 Zobrazit plný text záznamu