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10.1021/ml100143q

http://scihub22266oqcxt.onion/10.1021/ml100143q
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C4007905!4007905!24900234
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suck abstract from ncbi


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pmid24900234      ACS+Med+Chem+Lett 2010 ; 1 (9): 478-82
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  • A Potent and Selective AMPK Activator That Inhibits de Novo Lipogenesis #MMPMID24900234
  • Gómez-Galeno JE; Dang Q; Nguyen TH; Boyer SH; Grote MP; Sun Z; Chen M; Craigo WA; van Poelje PD; MacKenna DA; Cable EE; Rolzin PA; Finn PD; Chi B; Linemeyer DL; Hecker SJ; Erion MD
  • ACS Med Chem Lett 2010[Dec]; 1 (9): 478-82 PMID24900234show ga
  • 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 (EC50 = 6 nM vs AMP EC50 = 6 ?M) and specificity. Phosphonate prodrugs of 2 inhibited de novo lipogenesis in cellular and animal models of hyperlipidemia.
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