title: Sirtuin 5: a review of structure, known inhibitors and clues for developing new inhibitors.
abstract: Sirtuins (SIRTs) are nicotinamide adenine dinucleotide (NAD+)-dependent protein deacetylases, which regulate important biological processes ranging from apoptosis, age-associated pathophysiologies, adipocyte and muscle differentiation, and energy expenditure to gluconeogenesis. Very recently, sirtuin 5 (SIRT5) has received considerable attention due to that it was found to have weak deacetylase activity but strong desuccinylase, demalonylase and deglutarylase activities, and it was also found to be associated with several human diseases such as cancer, Alzheimer's disease, and Parkinson's disease. In this review, we for the first time summarized the structure characteristics, known peptide and smallmolecule inhibitors of SIRT5, extracted some clues from current available information and introduced some feasible, practical in silico methods, which might be useful in further efforts to develop new SIRT5 inhibitors.
authors.affiliation: College of Food and Bioengineering, Xihua University, Sichuan, 610039, China.
authors.forename: Lingling
authors.initials: L
authors.lastname: Yang
authors.affiliation: College of Food and Bioengineering, Xihua University, Sichuan, 610039, China.
authors.forename: Xiaobo
authors.initials: X
authors.lastname: Ma
authors.affiliation: College of Food and Bioengineering, Xihua University, Sichuan, 610039, China.
authors.forename: Yanying
authors.initials: Y
authors.lastname: He
authors.affiliation: College of Food and Bioengineering, Xihua University, Sichuan, 610039, China.
authors.forename: Chen
authors.initials: C
authors.lastname: Yuan
authors.affiliation: College of Food and Bioengineering, Xihua University, Sichuan, 610039, China.
authors.forename: Quanlong
authors.initials: Q
authors.lastname: Chen
authors.affiliation: Key Laboratory of Drug Targeting and Drug Delivery System of Ministry of Education, West China School of Pharmacy, Sichuan University, Chengdu, 610041, China. liguobo@scu.edu.cn.
authors.forename: Guobo
authors.initials: G
authors.lastname: Li
authors.affiliation: College of Food and Bioengineering, Xihua University, Sichuan, 610039, China. chenxianggui@tom.com.
authors.forename: Xianggui
authors.initials: X
authors.lastname: Chen
mesh_terms: D000595:Amino Acid Sequence; D018360:Crystallography, X-Ray; D004791:Enzyme Inhibitors / Q000737:chemistry; D006801:Humans; D015394:Molecular Structure; D010455:Peptides / Q000737:chemistry; D017434:Protein Structure, Tertiary; D037761:Sirtuins / Q000037:antagonists & inhibitors* / Q000737:chemistry*; D013329:Structure-Activity Relationship
chemical_list: D004791:Enzyme Inhibitors; D010455:Peptides; D037761:Sirtuins
keywords: SIRT5 inhibitor; Sirtuin; computer-aided drug design; crystal structure; small-molecule inhibitors