Hardie DG, Ross FA, Hawley SA . AMPK: a nutrient and energy sensor that maintains energy homeostasis. Nat Rev Mol Cell Biol 2012; 13: 251–262.
Mihaylova MM, Shaw RJ . The AMPK signalling pathway coordinates cell growth, autophagy and metabolism. Nat Cell Biol 2011; 13: 1016–1023.
Vazquez-Martin A, Oliveras-Ferraros C, Menendez JA . The active form of the metabolic sensor: AMP-activated protein kinase (AMPK) directly binds the mitotic apparatus and travels from centrosomes to the spindle midzone during mitosis and cytokinesis. Cell Cycle 2009; 8: 2385–2398.
Salt I, Celler JW, Hawley SA, Prescott A, Woods A, Carling D et al. AMP-activated protein kinase: greater AMP dependence, and preferential nuclear localization, of complexes containing the alpha2 isoform. Biochem J 1998; 334 (Pt 1): 177–187.
Birk JB, Wojtaszewski JF . Predominant alpha2/beta2/gamma3 AMPK activation during exercise in human skeletal muscle. J Physiol 2006; 577 (Pt 3): 1021–1032.
Burwinkel B, Scott JW, Buhrer C, van Landeghem FK, Cox GF, Wilson CJ et al. Fatal congenital heart glycogenosis caused by a recurrent activating R531Q mutation in the gamma 2-subunit of AMP-activated protein kinase (PRKAG2), not by phosphorylase kinase deficiency. Am J Hum Genet 2005; 76: 1034–1049.
Steinberg GR, O'Neill HM, Dzamko NL, Galic S, Naim T, Koopman R et al. Whole body deletion of AMP-activated protein kinase {beta}2 reduces muscle AMPK activity and exercise capacity. J Biol Chem 2010; 285: 37198–37209.
Barnes BR, Marklund S, Steiler TL, Walter M, Hjalm G, Amarger V et al. The 5′-AMP-activated protein kinase gamma3 isoform has a key role in carbohydrate and lipid metabolism in glycolytic skeletal muscle. J Biol Chem 2004; 279: 38441–38447.
Hawley SA, Davison M, Woods A, Davies SP, Beri RK, Carling D et al. Characterization of the AMP-activated protein kinase kinase from rat liver and identification of threonine 172 as the major site at which it phosphorylates AMP-activated protein kinase. J Biol Chem 1996; 271: 27879–27887.
Stein SC, Woods A, Jones NA, Davison MD, Carling D . The regulation of AMP-activated protein kinase by phosphorylation. Biochem J 2000; 345 (Pt 3): 437–443.
Xiao B, Heath R, Saiu P, Leiper FC, Leone P, Jing C et al. Structural basis for AMP binding to mammalian AMP-activated protein kinase. Nature 2007; 449: 496–500.
Xiao B, Sanders MJ, Carmena D, Bright NJ, Haire LF, Underwood E et al. Structural basis of AMPK regulation by small molecule activators. Nat Commun 2013; 4: 3017.
Xiao B, Sanders MJ, Underwood E, Heath R, Mayer FV, Carmena D et al. Structure of mammalian AMPK and its regulation by ADP. Nature 2011; 472: 230–233.
Ignoul S, Eggermont J . CBS domains: structure, function, and pathology in human proteins. Am J Physiol Cell Physiol 2005; 289: C1369–C1378.
Viana R, Towler MC, Pan DA, Carling D, Viollet B, Hardie DG et al. A conserved sequence immediately N-terminal to the Bateman domains in AMP-activated protein kinase gamma subunits is required for the interaction with the beta subunits. J Biol Chem 2007; 282: 16117–16125.
Oakhill JS, Scott JW, Kemp BE . AMPK functions as an adenylate charge-regulated protein kinase. Trends Endocrinol Metab 2012; 23: 125–132.
Gowans GJ, Hawley SA, Ross FA, Hardie DG . AMP is a true physiological regulator of AMP-activated protein kinase by both allosteric activation and enhancing net phosphorylation. Cell Metab 2013; 18: 556–566.
Hawley SA, Boudeau J, Reid JL, Mustard KJ, Udd L, Makela TP et al. Complexes between the LKB1 tumor suppressor, STRAD alpha/beta and MO25 alpha/beta are upstream kinases in the AMP-activated protein kinase cascade. J Biol 2003; 2: 28.
Woods A, Dickerson K, Heath R, Hong SP, Momcilovic M, Johnstone SR et al. Ca2+/calmodulin-dependent protein kinase kinase-beta acts upstream of AMP-activated protein kinase in mammalian cells. Cell Metab 2005; 2: 21–33.
Hawley SA, Selbert MA, Goldstein EG, Edelman AM, Carling D, Hardie DG . 5′-AMP activates the AMP-activated protein kinase cascade, and Ca2+/calmodulin activates the calmodulin-dependent protein kinase I cascade, via three independent mechanisms. J Biol Chem 1995; 270: 27186–27191.
Davies SP, Helps NR, Cohen PT, Hardie DG . 5′-AMP inhibits dephosphorylation, as well as promoting phosphorylation, of the AMP-activated protein kinase. Studies using bacterially expressed human protein phosphatase-2C alpha and native bovine protein phosphatase-2AC. FEBS Lett 1995; 377: 421–425.
Oakhill JS, Steel R, Chen ZP, Scott JW, Ling N, Tam S et al. AMPK is a direct adenylate charge-regulated protein kinase. Science 2011; 332: 1433–1435.
Towler MC, Hardie DG . AMP-activated protein kinase in metabolic control and insulin signaling. Circ Res 2007; 100: 328–341.
Fogarty S, Hardie DG . Development of protein kinase activators: AMPK as a target in metabolic disorders and cancer. Biochim Biophys Acta 2010; 1804: 581–591.
Hardie DG . AMPK: a key regulator of energy balance in the single cell and the whole organism. Int J Obes (Lond) 2008; 32 (Suppl 4): S7–12.
Hardie DG . Energy sensing by the AMP-activated protein kinase and its effects on muscle metabolism. Proc Nutr Soc 2011; 70: 92–99.
Hardie DG . AMP-activated protein kinase: maintaining energy homeostasis at the cellular and whole-body levels. Annu Rev Nutr 2014; 34: 31–55.
Hardie DG . AMP-activated protein kinase: a master switch in glucose and lipid metabolism. Rev Endocr Metab Disord 2004; 5: 119–125.
Musi N, Goodyear LJ . Targeting the AMP-activated protein kinase for the treatment of type 2 diabetes. Curr Drug Targets Immune Endocr Metabol Disord 2002; 2: 119–127.
Musi N . AMP-activated protein kinase and type 2 diabetes. Curr Med Chem 2006; 13: 583–589.
Rehman G, Shehzad A, Khan AL, Hamayun M . Role of AMP-activated protein kinase in cancer therapy. Arch Pharm (Weinheim) 2014; 347: 457–468.
Alessi DR, Sakamoto K, Bayascas JR . LKB1-dependent signaling pathways. Annu Rev Biochem 2006; 75: 137–163.
Hemminki A . The molecular basis and clinical aspects of Peutz-Jeghers syndrome. Cell Mol Life Sci 1999; 55: 735–750.
Evans JM, Donnelly LA, Emslie-Smith AM, Alessi DR, Morris AD . Metformin and reduced risk of cancer in diabetic patients. Br Med J 2005; 330: 1304–1305.
Huang X, Wullschleger S, Shpiro N, McGuire VA, Sakamoto K, Woods YL et al. Important role of the LKB1-AMPK pathway in suppressing tumorigenesis in PTEN-deficient mice. Biochem J 2008; 412: 211–221.
Gwinn DM, Shackelford DB, Egan DF, Mihaylova MM, Mery A, Vasquez DS et al. AMPK phosphorylation of raptor mediates a metabolic checkpoint. Mol Cell 2008; 30: 214–226.
Inoki K, Zhu T, Guan KL . TSC2 mediates cellular energy response to control cell growth and survival. Cell 2003; 115: 577–590.
Hoppe S, Bierhoff H, Cado I, Weber A, Tiebe M, Grummt I et al. AMP-activated protein kinase adapts rRNA synthesis to cellular energy supply. Proc Natl Acad Sci USA 2009; 106: 17781–17786.
Jones RG, Plas DR, Kubek S, Buzzai M, Mu J, Xu Y et al. AMP-activated protein kinase induces a p53-dependent metabolic checkpoint. Mol Cell 2005; 18: 283–293.
Imamura K, Ogura T, Kishimoto A, Kaminishi M, Esumi H . Cell cycle regulation via p53 phosphorylation by a 5′-AMP activated protein kinase activator, 5-aminoimidazole- 4-carboxamide-1-beta-D-ribofuranoside, in a human hepatocellular carcinoma cell line. Biochem Biophys Res Commun 2001; 287: 562–567.
Liang J, Shao SH, Xu ZX, Hennessy B, Ding Z, Larrea M et al. The energy sensing LKB1-AMPK pathway regulates p27(kip1) phosphorylation mediating the decision to enter autophagy or apoptosis. Nat Cell Biol 2007; 9: 218–224.
Budanov AV, Karin M . p53 target genes sestrin1 and sestrin2 connect genotoxic stress and mTOR signaling. Cell 2008; 134: 451–460.
He C, Klionsky DJ . Regulation mechanisms and signaling pathways of autophagy. Annu Rev Genet 2009; 43: 67–93.
Kroemer G, Marino G, Levine B . Autophagy and the integrated stress response. Mol Cell 2010; 40: 280–293.
Mizushima N, Levine B . Autophagy in mammalian development and differentiation. Nat Cell Biol 2010; 12: 823–830.
Galluzzi L, Pietrocola F, Levine B, Kroemer G . Metabolic control of autophagy. Cell 2014; 159: 1263–1276.
Kim J, Kundu M, Viollet B, Guan KL . AMPK and mTOR regulate autophagy through direct phosphorylation of Ulk1. Nat Cell Biol 2011; 13: 132–141.
Egan DF, Shackelford DB, Mihaylova MM, Gelino S, Kohnz RA, Mair W et al. Phosphorylation of ULK1 (hATG1) by AMP-activated protein kinase connects energy sensing to mitophagy. Science 2011; 331: 456–461.
Kim J, Kim YC, Fang C, Russell RC, Kim JH, Fan W et al. Differential regulation of distinct Vps34 complexes by AMPK in nutrient stress and autophagy. Cell 2013; 152: 290–303.
Ha J, Guan KL, Kim J . AMPK and autophagy in glucose/glycogen metabolism. Mol Aspects Med 2015; 46: 46–62.
Singh R, Kaushik S, Wang Y, Xiang Y, Novak I, Komatsu M et al. Autophagy regulates lipid metabolism. Nature 2009; 458: 1131–1135.
Singh R, Xiang Y, Wang Y, Baikati K, Cuervo AM, Luu YK et al. Autophagy regulates adipose mass and differentiation in mice. J Clin Invest 2009; 119: 3329–3339.
Kim J, Shin J, Ha J . Screening methods for AMP-activated protein kinase modulators: a patent review. Expert Opin Ther Pat 2015; 25: 261–277.
Sinnett SE, Brenman JE . Past strategies and future directions for identifying AMP-activated protein kinase (AMPK) modulators. Pharmacol Ther 2014; 143: 111–118.
Hardie DG . AMP-activated protein kinase as a drug target. Annu Rev Pharmacol Toxicol 2007; 47: 185–210.
Sriwijitkamol A, Musi N . Advances in the development of AMPK-activating compounds. Expert Opin Drug Discov 2008; 3: 1167–1176.
Foretz M, Guigas B, Bertrand L, Pollak M, Viollet B . Metformin: from mechanisms of action to therapies. Cell Metab 2014; 20: 953–966.
Zhou G, Myers R, Li Y, Chen Y, Shen X, Fenyk-Melody J et al. Role of AMP-activated protein kinase in mechanism of metformin action. J Clin Invest 2001; 108: 1167–1174.
Owen MR, Doran E, Halestrap AP . Evidence that metformin exerts its anti-diabetic effects through inhibition of complex 1 of the mitochondrial respiratory chain. Biochem J 2000; 348 (Pt 3): 607–614.
Hawley SA, Ross FA, Chevtzoff C, Green KA, Evans A, Fogarty S et al. Use of cells expressing gamma subunit variants to identify diverse mechanisms of AMPK activation. Cell Metab 2010; 11: 554–565.
Foretz M, Hebrard S, Leclerc J, Zarrinpashneh E, Soty M, Mithieux G et al. Metformin inhibits hepatic gluconeogenesis in mice independently of the LKB1/AMPK pathway via a decrease in hepatic energy state. J Clin Invest 2010; 120: 2355–2369.
Fryer LG, Parbu-Patel A, Carling D . The Anti-diabetic drugs rosiglitazone and metformin stimulate AMP-activated protein kinase through distinct signaling pathways. J Biol Chem 2002; 277: 25226–25232.
LeBrasseur NK, Kelly M, Tsao TS, Farmer SR, Saha AK, Ruderman NB et al. Thiazolidinediones can rapidly activate AMP-activated protein kinase in mammalian tissues. Am J Physiol Endocrinol Metab 2006; 291: E175–E181.
Saha AK, Avilucea PR, Ye JM, Assifi MM, Kraegen EW, Ruderman NB . Pioglitazone treatment activates AMP-activated protein kinase in rat liver and adipose tissue in vivo. Biochem Biophys Res Commun 2004; 314: 580–585.
Brunmair B, Staniek K, Gras F, Scharf N, Althaym A, Clara R et al. Thiazolidinediones, like metformin, inhibit respiratory complex I: a common mechanism contributing to their antidiabetic actions? Diabetes 2004; 53: 1052–1059.
Baur JA, Pearson KJ, Price NL, Jamieson HA, Lerin C, Kalra A et al. Resveratrol improves health and survival of mice on a high-calorie diet. Nature 2006; 444: 337–342.
Park CE, Kim MJ, Lee JH, Min BI, Bae H, Choe W et al. Resveratrol stimulates glucose transport in C2C12 myotubes by activating AMP-activated protein kinase. Exp Mol Med 2007; 39: 222–229.
Ahn J, Lee H, Kim S, Park J, Ha T . The anti-obesity effect of quercetin is mediated by the AMPK and MAPK signaling pathways. Biochem Biophys Res Commun 2008; 373: 545–549.
Hwang JT, Park IJ, Shin JI, Lee YK, Lee SK, Baik HW et al. Genistein, EGCG, and capsaicin inhibit adipocyte differentiation process via activating AMP-activated protein kinase. Biochem Biophys Res Commun 2005; 338: 694–699.
Lee YS, Kim WS, Kim KH, Yoon MJ, Cho HJ, Shen Y et al. Berberine, a natural plant product, activates AMP-activated protein kinase with beneficial metabolic effects in diabetic and insulin-resistant states. Diabetes 2006; 55: 2256–2264.
Kim T, Davis J, Zhang AJ, He X, Mathews ST . Curcumin activates AMPK and suppresses gluconeogenic gene expression in hepatoma cells. Biochem Biophys Res Commun 2009; 388: 377–382.
Gledhill JR, Montgomery MG, Leslie AG, Walker JE . Mechanism of inhibition of bovine F1-ATPase by resveratrol and related polyphenols. Proc Natl Acad Sci USA 2007; 104: 13632–13637.
Zheng J, Ramirez VD . Inhibition of mitochondrial proton F0F1-ATPase/ATP synthase by polyphenolic phytochemicals. Br J Pharmacol 2000; 130: 1115–1123.
Turner N, Li JY, Gosby A, To SW, Cheng Z, Miyoshi H et al. Berberine and its more biologically available derivative, dihydroberberine, inhibit mitochondrial respiratory complex I: a mechanism for the action of berberine to activate AMP-activated protein kinase and improve insulin action. Diabetes 2008; 57: 1414–1418.
Jeong KJ, Kim GW, Chung SH . AMP-activated protein kinase: an emerging target for ginseng. J Ginseng Res 2014; 38: 83–88.
Shen L, Xiong Y, Wang DQ, Howles P, Basford JE, Wang J et al. Ginsenoside Rb1 reduces fatty liver by activating AMP-activated protein kinase in obese rats. J Lipid Res 2013; 54: 1430–1438.
Golbidi S, Badran M, Laher I . Diabetes and alpha lipoic acid. Front Pharmacol 2011; 2: 69.
Lee WJ, Song KH, Koh EH, Won JC, Kim HS, Park HS et al. Alpha-lipoic acid increases insulin sensitivity by activating AMPK in skeletal muscle. Biochem Biophys Res Commun 2005; 332: 885–891.
Lee Y, Naseem RH, Park BH, Garry DJ, Richardson JA, Schaffer JE et al. Alpha-lipoic acid prevents lipotoxic cardiomyopathy in acyl CoA-synthase transgenic mice. Biochem Biophys Res Commun 2006; 344: 446–452.
Lee WJ, Lee IK, Kim HS, Kim YM, Koh EH, Won JC et al. Alpha-lipoic acid prevents endothelial dysfunction in obese rats via activation of AMP-activated protein kinase. Arterioscler Thromb Vasc Biol 2005; 25: 2488–2494.
Shen QW, Zhu MJ, Tong J, Ren J, Du M . Ca2+/calmodulin-dependent protein kinase kinase is involved in AMP-activated protein kinase activation by alpha-lipoic acid in C2C12 myotubes. Am J Physiol Cell Physiol 2007; 293: C1395–C1403.
Kim MS, Park JY, Namkoong C, Jang PG, Ryu JW, Song HS et al. Anti-obesity effects of alpha-lipoic acid mediated by suppression of hypothalamic AMP-activated protein kinase. Nat Med 2004; 10: 727–733.
Choi SL, Kim SJ, Lee KT, Kim J, Mu J, Birnbaum MJ et al. The regulation of AMP-activated protein kinase by H(2)O(2). Biochem Biophys Res Commun 2001; 287: 92–97.
Wu Y, Viana M, Thirumangalathu S, Loeken MR . AMP-activated protein kinase mediates effects of oxidative stress on embryo gene expression in a mouse model of diabetic embryopathy. Diabetologia 2012; 55: 245–254.
Quintero M, Colombo SL, Godfrey A, Moncada S . Mitochondria as signaling organelles in the vascular endothelium. Proc Natl Acad Sci USA 2006; 103: 5379–5384.
Zmijewski JW, Banerjee S, Bae H, Friggeri A, Lazarowski ER, Abraham E . Exposure to hydrogen peroxide induces oxidation and activation of AMP-activated protein kinase. J Biol Chem 2010; 285: 33154–33164.
Kim EJ, Jung SN, Son KH, Kim SR, Ha TY, Park MG et al. Antidiabetes and antiobesity effect of cryptotanshinone via activation of AMP-activated protein kinase. Mol Pharmacol 2007; 72: 62–72.
Park IJ, Yang WK, Nam SH, Hong J, Yang KR, Kim J et al. Cryptotanshinone induces G1 cell cycle arrest and autophagic cell death by activating the AMP-activated protein kinase signal pathway in HepG2 hepatoma. Apoptosis 2014; 19: 615–628.
Kim HS, Hwang JT, Yun H, Chi SG, Lee SJ, Kang I et al. Inhibition of AMP-activated protein kinase sensitizes cancer cells to cisplatin-induced apoptosis via hyper-induction of p53. J Biol Chem 2008; 283: 3731–3742.
Lee M, Hwang JT, Yun H, Kim EJ, Kim MJ, Kim SS et al. Critical roles of AMP-activated protein kinase in the carcinogenic metal-induced expression of VEGF and HIF-1 proteins in DU145 prostate carcinoma. Biochem Pharmacol 2006; 72: 91–103.
Corton JM, Gillespie JG, Hawley SA, Hardie DG . 5-aminoimidazole-4-carboxamide ribonucleoside. A specific method for activating AMP-activated protein kinase in intact cells? Eur J Biochem 1995; 229: 558–565.
Sullivan JE, Brocklehurst KJ, Marley AE, Carey F, Carling D, Beri RK . Inhibition of lipolysis and lipogenesis in isolated rat adipocytes with AICAR, a cell-permeable activator of AMP-activated protein kinase. FEBS Lett 1994; 353: 33–36.
Marie S, Heron B, Bitoun P, Timmerman T, Van Den Berghe G, Vincent MF . AICA-ribosiduria: a novel, neurologically devastating inborn error of purine biosynthesis caused by mutation of ATIC. Am J Hum Genet 2004; 74: 1276–1281.
Beckers A, Organe S, Timmermans L, Vanderhoydonc F, Deboel L, Derua R et al. Methotrexate enhances the antianabolic and antiproliferative effects of 5-aminoimidazole-4-carboxamide riboside. Mol Cancer Ther 2006; 5: 2211–2217.
McGuire JJ, Haile WH, Yeh CC . 5-amino-4-imidazolecarboxamide riboside potentiates both transport of reduced folates and antifolates by the human reduced folate carrier and their subsequent metabolism. Cancer Res 2006; 66: 3836–3844.
Vincent MF, Marangos PJ, Gruber HE, Van den Berghe G . Inhibition by AICA riboside of gluconeogenesis in isolated rat hepatocytes. Diabetes 1991; 40: 1259–1266.
Vincent MF, Bontemps F, Van den Berghe G . Inhibition of glycolysis by 5-amino-4-imidazolecarboxamide riboside in isolated rat hepatocytes. Biochem J 1992; 281 (Pt 1): 267–272.
Cool B, Zinker B, Chiou W, Kifle L, Cao N, Perham M et al. Identification and characterization of a small molecule AMPK activator that treats key components of type 2 diabetes and the metabolic syndrome. Cell Metab 2006; 3: 403–416.
Scott JW, van Denderen BJ, Jorgensen SB, Honeyman JE, Steinberg GR, Oakhill JS et al. Thienopyridone drugs are selective activators of AMP-activated protein kinase beta1-containing complexes. Chem Biol 2008; 15: 1220–1230.
Moreno D, Knecht E, Viollet B, Sanz P . A769662, a novel activator of AMP-activated protein kinase, inhibits non-proteolytic components of the 26S proteasome by an AMPK-independent mechanism. FEBS Lett 2008; 582: 2650–2654.
Scott JW, Ling N, Issa SM, Dite TA, O'Brien MT, Chen ZP et al. Small molecule drug A-769662 and AMP synergistically activate naive AMPK independent of upstream kinase signaling. Chem Biol 2014; 21: 619–627.
Sanders MJ, Ali ZS, Hegarty BD, Heath R, Snowden MA, Carling D . Defining the mechanism of activation of AMP-activated protein kinase by the small molecule A-769662, a member of the thienopyridone family. J Biol Chem 2007; 282: 32539–32548.
Hawley SA, Fullerton MD, Ross FA, Schertzer JD, Chevtzoff C, Walker KJ et al. The ancient drug salicylate directly activates AMP-activated protein kinase. Science 2012; 336: 918–922.
O'Brien AJ, Villani LA, Broadfield LA, Houde VP, Galic S, Blandino G et al. Salicylate activates AMPK and synergizes with metformin to reduce the survival of prostate and lung cancer cells ex vivo through inhibition of de novo lipogenesis. Biochem J 2015; 469: 177–187.
Fullerton MD, Ford RJ, McGregor CP, LeBlond ND, Snider SA, Stypa SA et al. Salicylate improves macrophage cholesterol homeostasis via activation of Ampk. J Lipid Res 2015; 56: 1025–1033.
Ford RJ, Fullerton MD, Pinkosky SL, Day EA, Scott JW, Oakhill JS et al. Metformin and salicylate synergistically activate liver AMPK, inhibit lipogenesis and improve insulin sensitivity. Biochem J 2015; 468: 125–132.
Serizawa Y, Oshima R, Yoshida M, Sakon I, Kitani K, Goto A et al. Salicylate acutely stimulates 5′-AMP-activated protein kinase and insulin-independent glucose transport in rat skeletal muscles. Biochem Biophys Res Commun 2014; 453: 81–85.
Gomez-Galeno JE, Dang Q, Nguyen TH, Boyer SH, Grote MP, Sun Z et al. A potent and selective AMPK activator that inhibits de novo lipogenesis. ACS Med Chem Lett 2010; 1: 478–482.
Hunter RW, Foretz M, Bultot L, Fullerton MD, Deak M, Ross FA et al. Mechanism of action of compound-13: an alpha1-selective small molecule activator of AMPK. Chem Biol 2014; 21: 866–879.
Goransson O, McBride A, Hawley SA, Ross FA, Shpiro N, Foretz M et al. Mechanism of action of A-769662, a valuable tool for activation of AMP-activated protein kinase. J Biol Chem 2007; 282: 32549–32560.
Pang T, Zhang ZS, Gu M, Qiu BY, Yu LF, Cao PR et al. Small molecule antagonizes autoinhibition and activates AMP-activated protein kinase in cells. J Biol Chem 2008; 283: 16051–16060.
Jensen TE, Ross FA, Kleinert M, Sylow L, Knudsen JR, Gowans GJ et al. PT-1 selectively activates AMPK-gamma1 complexes in mouse skeletal muscle, but activates all three gamma subunit complexes in cultured human cells by inhibiting the respiratory chain. Biochem J 2015; 467: 461–472.
Zadra G, Photopoulos C, Tyekucheva S, Heidari P, Weng QP, Fedele G et al. A novel direct activator of AMPK inhibits prostate cancer growth by blocking lipogenesis. EMBO Mol Med 2014; 6: 519–538.
Yuan X, Cai C, Chen S, Yu Z, Balk SP . Androgen receptor functions in castration-resistant prostate cancer and mechanisms of resistance to new agents targeting the androgen axis. Oncogene 2014; 33: 2815–2825.
Higano CS, Crawford ED . New and emerging agents for the treatment of castration-resistant prostate cancer. Urol Oncol 2011; 29 (6 Suppl): S1–S8.
Swinnen JV, Ulrix W, Heyns W, Verhoeven G . Coordinate regulation of lipogenic gene expression by androgens: evidence for a cascade mechanism involving sterol regulatory element binding proteins. Proc Natl Acad Sci USA 1997; 94: 12975–12980.
Ettinger SL, Sobel R, Whitmore TG, Akbari M, Bradley DR, Gleave ME et al. Dysregulation of sterol response element-binding proteins and downstream effectors in prostate cancer during progression to androgen independence. Cancer Res 2004; 64: 2212–2221.
Menendez JA, Lupu R . Fatty acid synthase and the lipogenic phenotype in cancer pathogenesis. Nat Rev Cancer 2007; 7: 763–777.
Zadra G, Priolo C, Patnaik A, Loda M . New strategies in prostate cancer: targeting lipogenic pathways and the energy sensor AMPK. Clin Cancer Res 2010; 16: 3322–3328.
Hardie DG . AMPK: positive and negative regulation, and its role in whole-body energy homeostasis. Curr Opin Cell Biol 2015; 33: 1–7.
Yun H, Ha J . AMP-activated protein kinase modulators: a patent review (2006–2010). Expert Opin Ther Pat 2011; 21: 983–1005.
Giordanetto F, Karis D . Direct AMP-activated protein kinase activators: a review of evidence from the patent literature. Expert Opin Ther Pat 2012; 22: 1467–1477.
Benziane B, Bjornholm M, Lantier L, Viollet B, Zierath JR, Chibalin AV . AMP-activated protein kinase activator A-769662 is an inhibitor of the Na(+)-K(+)-ATPase. Am J Physiol Cell Physiol 2009; 297: C1554–C1566.
Santos CR, Schulze A . Lipid metabolism in cancer. FEBS J 2012; 279: 2610–2623.