摘要
Sirtuins是NAD^+依赖性的进化保守的脱乙酰酶家族,家族内不同蛋白在亚细胞定位和功能方面显示出多样性。Sirtuin 2(SIRT2)在全身组织器官中均有表达,富集于代谢相关组织,亚细胞定位显示其主要存在于细胞质中,并能穿梭于细胞核内,参与多种生理活动,尤其在调节代谢方面具有重要作用,是临床治疗代谢性疾病的潜在靶点。目前以SIRT2为靶点的特效药还处于抑制剂或激动剂研发阶段,尚未有相关靶向特效药物进入临床试验。总结近年来SIRT2对体内外代谢过程的调控作用、作用靶点和相关调节剂及其与代谢相关疾病的研究进展。
Sirtuins are NAD^+-dependent evolutionarily conserved families of deacetylases,and different proteins within the family show diversity in subcellular localization and function.Sirtuin 2(SIRT2)is expressed in whole body tissues and organs,and is enriched in metabolic related tissues.Subcellular localization shows that SIRT2 mainly exists in the cytoplasm and can shuttle into the nucleus and participate in various physiological activities,especially in regulating metabolism.An important role of SIRT2 is the potential target for clinical treatment of metabolic diseases.At present,the specific drug targeting SIRT2 is still in the development stage of inhibitors or agonists,and no related specific effects drugs have entered the clinical trial.This review summarizes the recent advances in the regulation of SIRT2 on metabolic processes in vitro and in vivo,targets and related inhibitors or agonists,and their progress in metabolic-related diseases.
作者
张一睿
阿基业
谢媛
ZHANG Yirui;A Jiye;XIE Yuan(Key Lab of Drug Metabolism and Pharmacokinetics,China Pharmaceutical University,Nanjing 210000,China)
出处
《药物评价研究》
CAS
2019年第3期392-401,共10页
Drug Evaluation Research
基金
国家自然科学基金面上项目(81673679)
