title: Human SIRT3 tripeptidic inhibitors containing N(ε)-thioacetyl-lysine.
abstract: Built upon our lead pan-SIRT1/2/3 tripeptidic inhibitors that contain the catalytic mechanism-based sirtuin inhibitory warhead N(ε)-thioacetyl-lysine, three of their analogs (i.e., 7, 9, and 19) were discovered in the current study to exhibit a significantly enhanced SIRT3 inhibitory selectivity while maintaining the SIRT3 inhibitory potency. These compounds represent novel lead compounds for developing more potent and selective SIRT3 inhibitors of the catalytic mechanism-based type.
authors.affiliation: School of Pharmacy, Jiangsu University, 301 Xuefu Road, Zhenjiang 212013, Jiangsu Province, PR China.
authors.forename: Bing
authors.initials: B
authors.lastname: Chen
authors.affiliation: School of Pharmacy, Jiangsu University, 301 Xuefu Road, Zhenjiang 212013, Jiangsu Province, PR China.
authors.forename: Juan
authors.initials: J
authors.lastname: Wang
authors.affiliation: School of Pharmacy, Jiangsu University, 301 Xuefu Road, Zhenjiang 212013, Jiangsu Province, PR China.
authors.forename: Yajun
authors.initials: Y
authors.lastname: Huang
authors.affiliation: School of Pharmacy, Jiangsu University, 301 Xuefu Road, Zhenjiang 212013, Jiangsu Province, PR China. Electronic address: wzheng@ujs.edu.cn.
authors.forename: Weiping
authors.initials: W
authors.lastname: Zheng
mesh_terms: D002384:Catalysis; D006801:Humans; D008239:Lysine / Q000031:analogs & derivatives* / Q000037:antagonists & inhibitors; D008958:Models, Molecular; D056566:Sirtuin 3 / Q000235:genetics* / Q000378:metabolism*; D037761:Sirtuins / Q000737:chemistry*
chemical_list: C513649:N(epsilon)-thioacetyllysine; C466093:SIRT3 protein, human; D056566:Sirtuin 3; D037761:Sirtuins; D008239:Lysine
keywords: Deacetylation; Deacylation; Inhibitor; N(ε)-thioacetyl-lysine; SIRT3; Sirtuin