Discovery of MK-8722: A Systemic, Direct Pan-Activator of AMP-Activated Protein Kinase.
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SUBMITTER: Feng D
PROVIDER: S-EPMC5767883 | biostudies-literature | 2018 Jan
REPOSITORIES: biostudies-literature
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Discovery of MK-8722: A Systemic, Direct Pan-Activator of AMP-Activated Protein Kinase.
Feng Danqing D Biftu Tesfaye T Romero F Anthony FA Kekec Ahmet A Dropinski James J Kassick Andrew A Xu Shiyao S Kurtz Marc M MM Gollapudi Anantha A Shao Qing Q Yang Xiaodong X Lu Ku K Zhou Gaochao G Kemp Daniel D Myers Robert W RW Guan Hong-Ping HP Trujillo Maria E ME Li Cai C Weber Ann A Sebhat Iyassu K IK
ACS medicinal chemistry letters 20171201 1
5'-Adenosine monophosphate-activated protein kinase (AMPK) is a key regulator of mammalian energy homeostasis and has been implicated in mediating many of the beneficial effects of exercise and weight loss including lipid and glucose trafficking. As such, the enzyme has long been of interest as a target for the treatment of Type 2 Diabetes Mellitus. We describe the optimization of β1-selective, liver-targeted AMPK activators and their evolution into systemic pan-activators capable of acutely low ...[more]
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