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DOI | 10.1126/science.aah5582 |
Systemic pan-AMPK activator MK-8722 improves glucose homeostasis but induces cardiac hypertrophy | |
Myers, Robert W.1; Guan, Hong-Ping2; Ehrhart, Juliann3; Petrov, Aleksandr2; Prahalada, Srinivasa3; Tozzo, Effie2; Yang, Xiaodong2; Kurtz, Marc M.; Trujillo, Maria1; Trotter, Dinko Gonzalez4; Feng, Danqing5; Xu, Shiyao6; Eiermann, George; Holahan, Marie A.4; Rubins, Daniel4; Conarello, Stacey1; Niu, Xiaoda1; Souza, Sandra C.2; Miller, Corin4; Liu, Jinqi2; Lu, Ku2; Feng, Wen1; Li, Ying2; Painter, Ronald E.1; Milligan, James A.1; He, Huaibing; Liu, Franklin2; Ogawa, Aimie1; Wisniewski, Douglas1; Rohm, Rory J.2; Wang, Liyang1; Bunzel, Michelle; Qian, Ying2; Zhu, Wei2; Wang, Hongwu5; Bennet, Bindu3; Scheuch, Lisa LaFranco3; Fernandez, Guillermo E.3; Li, Cai1; Klimas, Michael4; Zhou, Gaochao1; van Heek, Margaret; Biftu, Tesfaye5; Weber, Ann5; Kelley, David E.2; Thornberry, Nancy2; Erion, Mark D.2; Kemp, Daniel M.2; Sebhat, Iyassu K.5 | |
2017-08-04 | |
发表期刊 | SCIENCE |
ISSN | 0036-8075 |
EISSN | 1095-9203 |
出版年 | 2017 |
卷号 | 357期号:6350页码:507-511 |
文章类型 | Article |
语种 | 英语 |
国家 | USA |
英文摘要 | 5'-Adenosine monophosphate-activated protein kinase (AMPK) is a master regulator of energy homeostasis in eukaryotes. Despite three decades of investigation, the biological roles of AMPK and its potential as a drug target remain incompletely understood, largely because of a lack of optimized pharmacological tools. We developed MK-8722, a potent, direct, allosteric activator of all 12 mammalian AMPK complexes. In rodents and rhesus monkeys, MK-8722-mediated AMPK activation in skeletal muscle induced robust, durable, insulin-independent glucose uptake and glycogen synthesis, with resultant improvements in glycemia and no evidence of hypoglycemia. These effects translated across species, including diabetic rhesus monkeys, but manifested with concomitant cardiac hypertrophy and increased cardiac glycogen without apparent functional sequelae. |
领域 | 地球科学 ; 气候变化 ; 资源环境 |
收录类别 | SCI-E |
WOS记录号 | WOS:000406840100039 |
WOS关键词 | PROTEIN-KINASE ; ENERGY HOMEOSTASIS ; METABOLIC SYNDROME ; GLYCOGEN-STORAGE ; MECHANISMS ; EXERCISE ; DISEASE ; HEALTH ; HEART ; MICE |
WOS类目 | Multidisciplinary Sciences |
WOS研究方向 | Science & Technology - Other Topics |
URL | 查看原文 |
引用统计 | |
文献类型 | 期刊论文 |
条目标识符 | http://119.78.100.173/C666/handle/2XK7JSWQ/196608 |
专题 | 地球科学 资源环境科学 气候变化 |
作者单位 | 1.Merck Res Labs, In Vitro Pharmacol, Kenilworth, NJ 07033 USA; 2.Merck Res Labs, Biol Discovery, Kenilworth, NJ 07033 USA; 3.Merck Res Labs, Safety Assessment & Lab Anim Resources, West Point, PA 19486 USA; 4.Merck Res Labs, Translat Imaging & Biomarkers Dept, West Point, PA 19486 USA; 5.Merck Res Labs, Med Chem, Kenilworth, NJ 07033 USA; 6.Merck Res Labs, PPDM Preclin ADME Dept, Kenilworth, NJ 07033 USA |
推荐引用方式 GB/T 7714 | Myers, Robert W.,Guan, Hong-Ping,Ehrhart, Juliann,et al. Systemic pan-AMPK activator MK-8722 improves glucose homeostasis but induces cardiac hypertrophy[J]. SCIENCE,2017,357(6350):507-511. |
APA | Myers, Robert W..,Guan, Hong-Ping.,Ehrhart, Juliann.,Petrov, Aleksandr.,Prahalada, Srinivasa.,...&Sebhat, Iyassu K..(2017).Systemic pan-AMPK activator MK-8722 improves glucose homeostasis but induces cardiac hypertrophy.SCIENCE,357(6350),507-511. |
MLA | Myers, Robert W.,et al."Systemic pan-AMPK activator MK-8722 improves glucose homeostasis but induces cardiac hypertrophy".SCIENCE 357.6350(2017):507-511. |
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