Journal
ACS MEDICINAL CHEMISTRY LETTERS
Volume 1, Issue 9, Pages 478-482Publisher
AMER CHEMICAL SOC
DOI: 10.1021/ml100143q
Keywords
5-(5-Hydroxy-isoxazol-3-yl)-furan-2-phosphonic acid; AMPK activator; lipogenesis; hepatocytes
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AMP-activated protein kinase (AMPK) is a heterotrimeric kinase that regulates cellular. energy metabolism by affecting energy-consuming pathways such as de novo. lipid biosynthesis and glucose production as well as energy-producing pathways such as lipid oxidation and glucose uptake. Accordingly, compounds that activate AMPK represent potential drug candidates for the treatment of hyperlipidemia and type 2 diabetes. Screening of a proprietary library of AMP mimetics identified the phosphonic acid 2 that bears little structural resemblance to AMP but is capable of activating AMPK with high potency (EC(50) = 6 nM vs AMP EC(50) = 6 mu M) and specificity. Phosphonate prodrugs of 2 inhibited de novo lipogenesis In cellular and animal models of hyperlipidemia.
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