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Inhibitors of diacylglycerol acyltransferase: a review of 2008 patents

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Pages 19-29 | Published online: 20 Dec 2009

Bibliography

  • Bansal S, Buring JE, Rifai N, Fasting compared with nonfasting triglycerides and risk of cardiovascular events in women. JAMA 2007;298(3):309-16
  • Nordestgaard BG, Benn M, Tybjaerg-Hansen A. Nonfasting triglycerides and risk of myocardial infarction, ischemic heart disease, and death in men and women. JAMA 2007:298(3):299-308
  • Capeau J. Insulin resistance and steatosis in humans. Diabetes Metab 2008;34(6 Pt 2):649-57
  • Kennedy EP. Metabolism of lipids. Annu Rev Biochem 1957;26:119-48
  • Kayden HJ, Senior JR, Mattson FH. The monoglyceride pathway of fat absorption in man. J Clin Invest 1967;46(11):1695-703
  • Yen CL, Stone SJ, Koliwad S, Thematic Review Series: Glycerolipids. DGAT enzymes and triacylglycerol biosynthesis. J Lipid Res 2008;49(11):2283-301
  • Cases S, Smith SJ, Zheng Y-W, Identification of a gene encoding an acyl CoA:diacylglycerol acyltransferase, a key enzyme in triacylglycerol synthesis. Proc Natl Acad Sci USA 1998;95(22):13018-23
  • Cases S, Stone SJ, Zhou P, Cloning of DGAT2, a second mammalian diacylglycerol acyltransferase, and related family members. J Biol Chem 2001;276(42):38870-6
  • Smith SJ, Cases S, Jensen DR, Obesity resistance and multiple mechanisms of triglyceride synthesis in mice lacking DGAT. Nat Genet 2000;25(1):87-90
  • Chen HC, Smith SJ, Ladha Z, Increased insulin and leptin sensitivity in mice lacking acyl CoA:diacylglycerol acyltransferase 1. J Clin Invest 2002;109(8):1049-55
  • Chen HC, Rao M, Sajan MP, Role of adipocyte-derived factors in enhancing insulin signaling in skeletal muscle and white adipose tissue of mice lacking Acyl CoA:diacylglycerol acyltransferase 1. Diabetes 2004;53(6):1445-51
  • Chen HC, Ladha Z, Smith SJ, Analysis of energy expenditure at different ambient temperatures in mice lacking DGAT-1. Am J Physiol Endocrinol Metab 2003;284(1):E213-8
  • Buhman KK, Smith SJ, Stone SJ, DGAT-1 is not essential for intestinal triacylglycerol absorption or chylomicron synthesis. J Biol Chem 2002;277(28):25474-9
  • Bayer . Preparation and use of aryl alkyl acid derivatives for the treatment of obesity. US07091228; 2004
  • Zhao G, Souers AJ, Voorbach M, Validation of diacyl glycerolacyltransferase I as a novel target for the treatment of obesity and dyslipidemia using a potent and selective small molecule inhibitor. J Med Chem 2008;51(3):380-3
  • Birch AM, Birtles S, Buckett LK, Discovery of a potent, selective, and orally efficacious pyrimidinooxazinyl bicyclooctaneacetic acid diacylglycerol acyltransferase-1 inhibitor. J Med Chem 2009;52(6):1558-68
  • King AJ, Segreti JA, Larson KJ, Diacylglycerol acyltransferase 1 (DGAT-1) inhibition lowers serum triglycerides in the Zucker fatty rat and the hyperlipidemic hamster. J Pharmacol Exp Ther 2009;330(2):526-31
  • Chen HC, Smith SJ, Tow B, Leptin modulates the effects of acyl CoA:diacylglycerol acyltransferase deficiency on murine fur and sebaceous glands. J Clin Invest 2002;109(2):175-81
  • Cases S, Zhou P, Shillingford JM, Development of the mammary gland requires DGAT-1 expression in stromal and epithelial tissues. Development 2004;131(13):3047-55
  • Chen HC, Farese RV Jr. Inhibition of triglyceride synthesis as a treatment strategy for obesity: lessons from DGAT-1-deficient mice. Arterioscler Thromb Vasc Biol 2005;25(3):482-6
  • Stone SJ, Myers HM, Watkins SM, Lipopenia and skin barrier abnormalities in DGAT2-deficient mice. J Biol Chem 2004;279(12):11767-76
  • Yu XX, Liu ZX, Morino K, Antisense oligonucleotide reduction of DGAT2 expression improves hepatic steatosis and hyperlipidemia in obese mice. Hepatology 2005;42(2):362-71
  • Liu Y, Millar JS, Cromley DA, Knockdown of acyl-CoA:diacylglycerol acyltransferase 2 with antisense oligonucleotide reduces VLDL TG and ApoB secretion in mice. Biochim Biophys Acta 2008;1781(3):97-104
  • Choi CS, Savage DB, Kulkarni A, Suppression of diacylglycerol acyltransferase-2 (DGAT2), but not DGAT-1, with antisense oligonucleotides reverses diet-induced hepatic steatosis and insulin resistance. J Biol Chem 2007;282(31):22678-88
  • Yamaguchi K, Liu Y, McCall S, Inhibiting triglyceride synthesis improves hepatic steatosis but exacerbates liver damage and fibrosis in obese mice with nonalcoholic steatohepatitis. Hepatology 2007;45(6):1366-74
  • Hubbard BK, Gilmore TA, Serrano-Wu MH. Antisense and small-molecule modulation of diacylglycerol acyltransferase. Expert Opin Ther Patent 2007;17:1331-9
  • Roche . Diacylglycerol acyltransferase inhibitors. WO2006120125; 2006
  • Roche. Diacylglycerol acyltransferase inhibitors. WO2007060140; 2007
  • Roche. Inhibitors of diacylglycerol acyltransferase. WO2006082010; 2006
  • Roche. Diacylglycerol acyltransferase inhibitors. WO2008141976; 2008
  • Takeda. Amide compounds. WO2008011130; 2008
  • Takeda. Amide compounds. WO2008011131; 2008
  • Astrazeneca. Oxadiazole derivatives as DGAT inhibitors. WO2006134317; 2006
  • BMS. Use of thianecarboxamides as DGAT inhbitors. US20080090876; 2008
  • Janssen. Piperidine/piperazine derivatives. WO2008148840; 2008
  • Janssen. Piperidine/piperazine derivatives. WO2008148849; 2008
  • Janssen. Piperidine/piperazine derivatives. WO2008148868; 2008
  • Janssen. Piperidine/piperazine derivatives. WO2008148851; 2008
  • Abbott. Inhibitors of diacyl O-acyltransferase type I enzyme. US2007069112; 2007
  • Abbott. Inhibitors of diacyl O-acyltransferase type I enzyme. US20080015227; 2008
  • Abbott. Inhibitors of diacyl O-acyltransferase type I enzyme. US20080312282; 2008
  • Abbott. Inhibitors of diacyl O-acyltransferase type I enzyme. US20080182861; 2008
  • Abbott. Inhibitors of diacyl O-acyltransferase type I enzyme. US20080293713; 2008
  • Souers AJ, King AJ, Mittelstadt S, “DGAT-1 Inhibitors as Novel Therapeutics for Dyslipidemia” Western Regional ACS meeting, San Diego, 2008
  • Souers AJ. “DGAT-1 Inhibitors as Novel Therapeutics for Dyslipidemia” 237th National ACS meeting, Salt Lake City, 2009
  • Korea Research institute of bioscience and biotechnology. Composition for the prevention and treatment of metabolic disorder containing benzazole derivatives as an active ingredient. WO2008039008; 2008
  • Korea Research institute of bioscience and biotechnology. Indol derivatives, the method for preparing thereof and composition for the prevention and treatment of metabolic disorder containing the same as an active ingredient. WO2008039007; 2008
  • Bioactives. Prenylflavonoid formulations. WO2007016578; 2007
  • Bioactives. Methods and compositions for treating dyslipidemia. WO2008095189; 2008
  • ISIS. Modulation of diacylglycerol acyltransferase 2 expression. WO2004094618; 2004
  • ISIS. Modulation of diacylglycerol acyltransferase 2 expression. US20050272680; 2005
  • ISIS. Compositions and their uses directed to diacylglycerol acyltransferase I. WO2008019351; 2008
  • Tularik and Japan Tobacco. Fused and bicyclic nitrogen-containing heterocycles. WO2004047755; 2004
  • Available from: http://pharma.bayer.com/scripts/pages/en/news_room/news_room/archive/newsroom_archive26.php
  • Available from: http://mediaroom.pfizer.com/portal/site/pfizer/index.jsp?ndmViewId=news_view&newsId=20070827005440&newsLang=en
  • Chia CW, Egan JM. Biology and therapeutic potential of GLP-1 in the treatment of diabetes. Drug Discov Today 2005;2(3):295-01
  • Shih MYS, Kane MA, Zhou P, Retinol esterification by DGAT1 is essential for retinoid homeostasis in murine skin. J Biol Chem 2008;284(7):4292-9
  • Sankyo. Medicine containing urea derivative. JP2007191471; 2007
  • Mucke H, Yeates C, Norman P. Patent alert. Current Opin Invest Drugs. 2006;7(9):781-88

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