title: A mechanism-based potent sirtuin inhibitor containing Nε-thiocarbamoyl-lysine (TuAcK).
abstract: In the current study, we have identified N(ε)-thiocarbamoyl-lysine (TuAcK) as a general sirtuin inhibitory warhead which was shown to be able to confer potent sirtuin inhibition. This inhibition was also shown to be mechanism-based in that the TuAck residue was able to be processed by a sirtuin enzyme with the formation of a stalled S-alkylamidate intermediate.
authors.affiliation: Department of Chemistry, University of Akron, Akron, OH 44325, USA.
authors.forename: Brett M
authors.initials: BM
authors.lastname: Hirsch
authors.forename: Yujun
authors.initials: Y
authors.lastname: Hao
authors.forename: Xiaopeng
authors.initials: X
authors.lastname: Li
authors.forename: Chrys
authors.initials: C
authors.lastname: Wesdemiotis
authors.forename: Zhenghe
authors.initials: Z
authors.lastname: Wang
authors.forename: Weiping
authors.initials: W
authors.lastname: Zheng
mesh_terms: D004791:Enzyme Inhibitors / Q000138:chemical synthesis / Q000737:chemistry / Q000494:pharmacology*; D008239:Lysine / Q000031:analogs & derivatives / Q000737:chemistry / Q000494:pharmacology*; D015394:Molecular Structure; D037761:Sirtuins / Q000037:antagonists & inhibitors*; D013237:Stereoisomerism; D013329:Structure-Activity Relationship; D013859:Thiocarbamates / Q000138:chemical synthesis / Q000737:chemistry / Q000494:pharmacology*
chemical_list: D004791:Enzyme Inhibitors; D013859:Thiocarbamates; D037761:Sirtuins; D008239:Lysine