메뉴 건너뛰기




Volumn 14, Issue 6, 2012, Pages 511-517

Biological and functional characteristics of a novel low-molecular weight antagonist of glucose-dependent insulinotropic polypeptide receptor, SKL-14959, in vitro and in vivo

Author keywords

GIP; GIP receptor antagonist; Glucose homeostasis; Insulin secretion; Lipase activity; Lipid homeostasis

Indexed keywords

CYCLIC AMP; GLUCAGON LIKE PEPTIDE 1; GLUCOSE; GLUCOSE DEPENDENT INSULINOTROPIC POLYPEPTIDE RECEPTOR; LIPOPROTEIN LIPASE; LIVER TRIACYLGLYCEROL LIPASE; RECEPTOR; RECEPTOR BLOCKING AGENT; SKL 14959; TRIACYLGLYCEROL; UNCLASSIFIED DRUG;

EID: 84862804002     PISSN: 14628902     EISSN: 14631326     Source Type: Journal    
DOI: 10.1111/j.1463-1326.2011.01555.x     Document Type: Article
Times cited : (19)

References (42)
  • 2
    • 0014811685 scopus 로고
    • Further purification of a polypeptide demonstrating enterogastrone activity.
    • Brown JC, Dryburgh JR. Further purification of a polypeptide demonstrating enterogastrone activity. J Physiol 1970; 209: 57-64.
    • (1970) J Physiol , vol.209 , pp. 57-64
    • Brown, J.C.1    Dryburgh, J.R.2
  • 3
    • 0018758893 scopus 로고
    • The incretin concept today.
    • Creutzfeldt W. The incretin concept today. Diabetologia 1979; 16: 75-85.
    • (1979) Diabetologia , vol.16 , pp. 75-85
    • Creutzfeldt, W.1
  • 4
    • 0023434193 scopus 로고
    • Sequence of an intestinal cDNA encoding human gastric inhibitory polypeptide precursor.
    • Takeda J, Seino Y, Tanaka K et al. Sequence of an intestinal cDNA encoding human gastric inhibitory polypeptide precursor. Proc Natl Acad Sci U S A 1987; 84: 7005-7008.
    • (1987) Proc Natl Acad Sci U S A , vol.84 , pp. 7005-7008
    • Takeda, J.1    Seino, Y.2    Tanaka, K.3
  • 5
    • 0027136670 scopus 로고
    • Gastric inhibitory polypeptide receptor, a member of the seretin-vasoactive intestinal peptide receptor family, is widely distributed in peripheral organs and the brain.
    • Usdin TB, Mezey E, Button DC, Brownstein MJ, Bonner TI. Gastric inhibitory polypeptide receptor, a member of the seretin-vasoactive intestinal peptide receptor family, is widely distributed in peripheral organs and the brain. Endocrinology 1993; 133: 2861-2870.
    • (1993) Endocrinology , vol.133 , pp. 2861-2870
    • Usdin, T.B.1    Mezey, E.2    Button, D.C.3    Brownstein, M.J.4    Bonner, T.I.5
  • 7
    • 0028847462 scopus 로고
    • Human gastric inhibitory polypeptide receptor cloning of the gene (GIPR) and cDNA.
    • Yamada Y, Hayami T, Nakamura K, Kaisaki P, Someya Y. Human gastric inhibitory polypeptide receptor cloning of the gene (GIPR) and cDNA. Genomics 1995; 29: 773-776.
    • (1995) Genomics , vol.29 , pp. 773-776
    • Yamada, Y.1    Hayami, T.2    Nakamura, K.3    Kaisaki, P.4    Someya, Y.5
  • 8
    • 13344293675 scopus 로고    scopus 로고
    • Expression and functional activity of glucagon, glucagon-like peptide I, and glucose-dependent insulinotropic peptide receptors in rat pancreatic islet cells.
    • Moens K, Heimberg H, Flamez D, Huypens P, Quartier E. Expression and functional activity of glucagon, glucagon-like peptide I, and glucose-dependent insulinotropic peptide receptors in rat pancreatic islet cells. Diabetes 1996; 45: 257-261.
    • (1996) Diabetes , vol.45 , pp. 257-261
    • Moens, K.1    Heimberg, H.2    Flamez, D.3    Huypens, P.4    Quartier, E.5
  • 9
    • 0029082308 scopus 로고
    • Functional expression of the rat pancreatic islet glucose-dependent insulinotropic polypeptide receptor: ligand binding and intracellular signaling properties.
    • Wheeler MB, Gelling RW, Mcintosh CH, Georgiou J, Brown JC. Functional expression of the rat pancreatic islet glucose-dependent insulinotropic polypeptide receptor: ligand binding and intracellular signaling properties. Endocrinology 1995; 136: 4629-4639.
    • (1995) Endocrinology , vol.136 , pp. 4629-4639
    • Wheeler, M.B.1    Gelling, R.W.2    Mcintosh, C.H.3    Georgiou, J.4    Brown, J.C.5
  • 10
    • 0018672563 scopus 로고
    • Gastric inhibitory polypeptide enhanced lipoprotein lipase activity in cultured preadipocyte.
    • Eckel RH, Fujimoto WY, Brunzell JD. Gastric inhibitory polypeptide enhanced lipoprotein lipase activity in cultured preadipocyte. Diabetes 1979; 28: 1141-1142.
    • (1979) Diabetes , vol.28 , pp. 1141-1142
    • Eckel, R.H.1    Fujimoto, W.Y.2    Brunzell, J.D.3
  • 11
    • 0028855353 scopus 로고
    • Investigations into the actions of glucose-dependent insulinotropic polypeptide and glucagon-like peptide-1(7-36) amide on lipoprotein lipase activity in explants of rat adipose tissue.
    • Knapper JM, Puddicombe SM, Morgan LM, Fletcher JM. Investigations into the actions of glucose-dependent insulinotropic polypeptide and glucagon-like peptide-1(7-36) amide on lipoprotein lipase activity in explants of rat adipose tissue. Nutrition 1995; 125: 183-188.
    • (1995) Nutrition , vol.125 , pp. 183-188
    • Knapper, J.M.1    Puddicombe, S.M.2    Morgan, L.M.3    Fletcher, J.M.4
  • 12
    • 34247880256 scopus 로고    scopus 로고
    • Activation of lipoprotein lipase by glucose-dependent insulinotropic polypeptide in adipocytes.
    • Kim SJ, Nian C, Mclntosh CH. Activation of lipoprotein lipase by glucose-dependent insulinotropic polypeptide in adipocytes. J Biol Chem 2007; 282: 8557-8567.
    • (2007) J Biol Chem , vol.282 , pp. 8557-8567
    • Kim, S.J.1    Nian, C.2    Mclntosh, C.H.3
  • 13
    • 0024271044 scopus 로고
    • Effects of gastric inhibitory polypeptide on glucose and lipids metabolism of isolated rat adipocytes.
    • Hauner H, Glatting G, Kaminska D, Pfeiffer EF. Effects of gastric inhibitory polypeptide on glucose and lipids metabolism of isolated rat adipocytes. Ann Nutr Metab 1988; 32: 282-288.
    • (1988) Ann Nutr Metab , vol.32 , pp. 282-288
    • Hauner, H.1    Glatting, G.2    Kaminska, D.3    Pfeiffer, E.F.4
  • 14
    • 33846893661 scopus 로고    scopus 로고
    • Glucose-dependent insulinotropic polypeptide modulates adipocyte lipolysis and reesterification.
    • Getty-Kaushik L, Song DH, Boylan MO, Corkey BE, Micheal Wolfe M. Glucose-dependent insulinotropic polypeptide modulates adipocyte lipolysis and reesterification. Obesity 2006; 14: 1124-1130.
    • (2006) Obesity , vol.14 , pp. 1124-1130
    • Getty-Kaushik, L.1    Song, D.H.2    Boylan, M.O.3    Corkey, B.E.4    Micheal Wolfe, M.5
  • 15
    • 0023494098 scopus 로고
    • Hypersensitivity of adipose tissue to gastric inhibitory polypeptide action in the obese zucker rat.
    • Beck B, Max JP. Hypersensitivity of adipose tissue to gastric inhibitory polypeptide action in the obese zucker rat. Cell Mol Biol 1987; 33: 555-562.
    • (1987) Cell Mol Biol , vol.33 , pp. 555-562
    • Beck, B.1    Max, J.P.2
  • 16
    • 0025808278 scopus 로고
    • Effect of the entero-pancreatic hormones, gastric inhibitory polypeptide and glucagon-like polypeptide-1(7-36) amide, on fatty acid synthesis in explants of rat adipose tissue.
    • Oben J, Morgan L, Fletcher J, Marks V. Effect of the entero-pancreatic hormones, gastric inhibitory polypeptide and glucagon-like polypeptide-1(7-36) amide, on fatty acid synthesis in explants of rat adipose tissue. J Endocrinol 1991; 130: 267-272.
    • (1991) J Endocrinol , vol.130 , pp. 267-272
    • Oben, J.1    Morgan, L.2    Fletcher, J.3    Marks, V.4
  • 17
    • 0019407932 scopus 로고
    • Effect of gastric inhibitory polypeptide on plasma levels of chylomicron triglycerides in dog.
    • Wasada T, McCorkle K, Harris V, Kawai K, Howard B. Effect of gastric inhibitory polypeptide on plasma levels of chylomicron triglycerides in dog. J Clin Invest 1981; 68: 1106-1107.
    • (1981) J Clin Invest , vol.68 , pp. 1106-1107
    • Wasada, T.1    McCorkle, K.2    Harris, V.3    Kawai, K.4    Howard, B.5
  • 18
    • 0025750777 scopus 로고
    • Effect of exogenous or endogenous gastric inhibitory polypeptide (GIP) on plasma triglyceride responses in rats.
    • Ebert R, Nauck M, Creutzfeldt W. Effect of exogenous or endogenous gastric inhibitory polypeptide (GIP) on plasma triglyceride responses in rats. Horm Metab Res 1991; 23: 517-521.
    • (1991) Horm Metab Res , vol.23 , pp. 517-521
    • Ebert, R.1    Nauck, M.2    Creutzfeldt, W.3
  • 19
    • 0018662619 scopus 로고
    • Impaired feedback control of fat induced gastric inhibitory polypeptide (GIP) secretion by insulin in obesity and glucose intolerance.
    • Ebert R, Frerichs H, Creutzfeldt W. Impaired feedback control of fat induced gastric inhibitory polypeptide (GIP) secretion by insulin in obesity and glucose intolerance. Eur J Clin Invest 1979; 9: 129-135.
    • (1979) Eur J Clin Invest , vol.9 , pp. 129-135
    • Ebert, R.1    Frerichs, H.2    Creutzfeldt, W.3
  • 20
    • 0017876434 scopus 로고
    • Gastric inhibitory polypeptide (GIP) and insulin in obesity: increased response to stimulation and defective feedback control of serum levels.
    • Creutzfeldt W, Ebert R, Willims B, Frerichs H, Brown JC. Gastric inhibitory polypeptide (GIP) and insulin in obesity: increased response to stimulation and defective feedback control of serum levels. Diabetologia 1979; 14: 15-24.
    • (1979) Diabetologia , vol.14 , pp. 15-24
    • Creutzfeldt, W.1    Ebert, R.2    Willims, B.3    Frerichs, H.4    Brown, J.C.5
  • 21
    • 0020411495 scopus 로고
    • Gastric inhibitory polypeptide release after oral glucose: Relationship to glucose intolerance, diabetes mellitus, and obesity.
    • Salera M, Giacomoni P, Pironi L, Cornia G, Capelli M, Marini A. Gastric inhibitory polypeptide release after oral glucose: Relationship to glucose intolerance, diabetes mellitus, and obesity. J Clin Endocrinol Metab 1982; 55: 329-336.
    • (1982) J Clin Endocrinol Metab , vol.55 , pp. 329-336
    • Salera, M.1    Giacomoni, P.2    Pironi, L.3    Cornia, G.4    Capelli, M.5    Marini, A.6
  • 22
    • 0021194112 scopus 로고
    • The enteric enhancement of glucose-stimulated insulin release: The role of GIP in aging, obesity, and non-insulin-dependent diabetes mellitus.
    • Elahi D, Andersen DK, Muller DC, Tobin JD, Brown JC, Andres R. The enteric enhancement of glucose-stimulated insulin release: The role of GIP in aging, obesity, and non-insulin-dependent diabetes mellitus. Diabetes 1984; 33: 950-957.
    • (1984) Diabetes , vol.33 , pp. 950-957
    • Elahi, D.1    Andersen, D.K.2    Muller, D.C.3    Tobin, J.D.4    Brown, J.C.5    Andres, R.6
  • 23
  • 24
    • 0036068322 scopus 로고    scopus 로고
    • Inhibition of gastric inhibitory polypeptide signaling prevents obesity.
    • Miyawaki K, Yamada Y, Ban N, Ihara Y, Tsukiyama K. Inhibition of gastric inhibitory polypeptide signaling prevents obesity. Nat Med 2002; 8: 738-742.
    • (2002) Nat Med , vol.8 , pp. 738-742
    • Miyawaki, K.1    Yamada, Y.2    Ban, N.3    Ihara, Y.4    Tsukiyama, K.5
  • 25
    • 34447127048 scopus 로고    scopus 로고
    • Chemical gastric inhibitory polypeptide receptor antagonism protects against obesity, insulin resistance, glucose intolerance and associated disturbances in mice fed high-fat and cafeteria diets.
    • Gault VA, McClean PL, Cassidy RS, Irwin N, Flatt PR. Chemical gastric inhibitory polypeptide receptor antagonism protects against obesity, insulin resistance, glucose intolerance and associated disturbances in mice fed high-fat and cafeteria diets. Diabetologia 2007; 50: 1752-1762.
    • (2007) Diabetologia , vol.50 , pp. 1752-1762
    • Gault, V.A.1    McClean, P.L.2    Cassidy, R.S.3    Irwin, N.4    Flatt, P.R.5
  • 26
    • 34249941340 scopus 로고    scopus 로고
    • Early administration of the glucose-dependent insulinotropic polypeptide receptor antagonist (Pro3)GIP prevents the development of diabetes and related metabolic abnormalities associated with genetically inherited obesity in ob/ob mice.
    • Irwin N, McClean PL, O'Harte FP, Gault VA, Harriott P, Flatt PR. Early administration of the glucose-dependent insulinotropic polypeptide receptor antagonist (Pro3)GIP prevents the development of diabetes and related metabolic abnormalities associated with genetically inherited obesity in ob/ob mice. Diabetologia 2007; 50: 1532-1540.
    • (2007) Diabetologia , vol.50 , pp. 1532-1540
    • Irwin, N.1    McClean, P.L.2    O'Harte, F.P.3    Gault, V.A.4    Harriott, P.5    Flatt, P.R.6
  • 27
    • 68449083816 scopus 로고    scopus 로고
    • Evidence for benefical effects of compromised gastric inhibitory polypeptide action in obesity-related diabetes and possible therapeutic implications.
    • Irwin N, Flatt PR. Evidence for benefical effects of compromised gastric inhibitory polypeptide action in obesity-related diabetes and possible therapeutic implications. Diabetologia 2009; 52: 1724-1731.
    • (2009) Diabetologia , vol.52 , pp. 1724-1731
    • Irwin, N.1    Flatt, P.R.2
  • 28
    • 1442321740 scopus 로고    scopus 로고
    • Evidence that the major degradation product of glucose-dependent insulinotropic polypeptide, GIP(3-42), is a GIP receptor antagonist in vivo.
    • Gault VA, Parker JC, Harriott P, Flatt PR, O'Harte FP. Evidence that the major degradation product of glucose-dependent insulinotropic polypeptide, GIP(3-42), is a GIP receptor antagonist in vivo. J Endocrinol 2002; 175: 525-533.
    • (2002) J Endocrinol , vol.175 , pp. 525-533
    • Gault, V.A.1    Parker, J.C.2    Harriott, P.3    Flatt, P.R.4    O'Harte, F.P.5
  • 29
    • 0029834106 scopus 로고    scopus 로고
    • Postprandial stimulation of insulin release by glucose-dependent insulinotropic polypeptide (GIP).
    • Tseng CC, Kieffer TJ, Jarboe LA, Usdin TB, Michael Wolfe M. Postprandial stimulation of insulin release by glucose-dependent insulinotropic polypeptide (GIP). J Clin Invest 1996; 98: 2440-2445.
    • (1996) J Clin Invest , vol.98 , pp. 2440-2445
    • Tseng, C.C.1    Kieffer, T.J.2    Jarboe, L.A.3    Usdin, T.B.4    Michael Wolfe, M.5
  • 30
    • 0036289106 scopus 로고    scopus 로고
    • Characterization of the cellular and metabolic effects of a novel enzyme-resistant antagonist of glucose-dependent insulinotropic polypeptide.
    • Gault VA, O'Harte PM, Harriott P, Flatt PR. Characterization of the cellular and metabolic effects of a novel enzyme-resistant antagonist of glucose-dependent insulinotropic polypeptide. Biochem Biophys Res Commun 2002; 290: 1420-1426.
    • (2002) Biochem Biophys Res Commun , vol.290 , pp. 1420-1426
    • Gault, V.A.1    O'Harte, P.M.2    Harriott, P.3    Flatt, P.R.4
  • 31
    • 10544249875 scopus 로고    scopus 로고
    • Identification of two missense mutations in the GIP receptor gene: a functional study and association analysis with NIDDM: no evidence of association with Japanese NIDDM subjects.
    • Kubota K, Yamada Y, Hayami T, Yasuda K, Someya Y. Identification of two missense mutations in the GIP receptor gene: a functional study and association analysis with NIDDM: no evidence of association with Japanese NIDDM subjects. Diabetes 1996; 45: 1701-1705.
    • (1996) Diabetes , vol.45 , pp. 1701-1705
    • Kubota, K.1    Yamada, Y.2    Hayami, T.3    Yasuda, K.4    Someya, Y.5
  • 33
    • 0033605578 scopus 로고    scopus 로고
    • Characterization of a novel, non-peptidyl antagonist of the human glucagon receptor.
    • Cascieri MA, Koch GE, Ber E, Sadowski SJ, Louizides D. Characterization of a novel, non-peptidyl antagonist of the human glucagon receptor. J Biol Chem 1999; 274: 8694-8697.
    • (1999) J Biol Chem , vol.274 , pp. 8694-8697
    • Cascieri, M.A.1    Koch, G.E.2    Ber, E.3    Sadowski, S.J.4    Louizides, D.5
  • 34
    • 0028893424 scopus 로고
    • Evidence that glucagon stimulates insulin secretion through its own receptor in rats.
    • Kawai K, Yokota C, Ohashi S, Watanabe Y, Yamashita K. Evidence that glucagon stimulates insulin secretion through its own receptor in rats. Diabetologia 1995; 38: 274-276.
    • (1995) Diabetologia , vol.38 , pp. 274-276
    • Kawai, K.1    Yokota, C.2    Ohashi, S.3    Watanabe, Y.4    Yamashita, K.5
  • 35
    • 0007866067 scopus 로고    scopus 로고
    • Glucose intolerance caused by a defect in the entero-insular axis: A study in gastric inhibitory polypeptide receptor knockout mice.
    • Miyawaki K, Yamada Y, Yano H, Seino Y. Glucose intolerance caused by a defect in the entero-insular axis: A study in gastric inhibitory polypeptide receptor knockout mice. Proc Natl Acad Sci U S A 1999; 96: 14843-14847.
    • (1999) Proc Natl Acad Sci U S A , vol.96 , pp. 14843-14847
    • Miyawaki, K.1    Yamada, Y.2    Yano, H.3    Seino, Y.4
  • 36
    • 23944463919 scopus 로고    scopus 로고
    • Gastric inhibitory polypeptide modulates adiposity and fat oxidation under diminished insulin action.
    • Zhou H, Yamada Y, Tsukiyama K, Miyawaki K. Gastric inhibitory polypeptide modulates adiposity and fat oxidation under diminished insulin action. Biochem Biophys Res Commun 2005; 335: 937-942.
    • (2005) Biochem Biophys Res Commun , vol.335 , pp. 937-942
    • Zhou, H.1    Yamada, Y.2    Tsukiyama, K.3    Miyawaki, K.4
  • 37
    • 0026606095 scopus 로고
    • Role of hepatic lipase in the catabolism of chylomicron remnants in the rat.
    • Grigilo S, Sultan F, Lagrange D. Role of hepatic lipase in the catabolism of chylomicron remnants in the rat. Diabete Metab 1992; 18: 150-155.
    • (1992) Diabete Metab , vol.18 , pp. 150-155
    • Grigilo, S.1    Sultan, F.2    Lagrange, D.3
  • 38
    • 0033965326 scopus 로고    scopus 로고
    • Differences in glucose-dependent insulinotropic polypeptide hormone and hepatic lipase in subjects of southern and northern Europe: implications for postprandial lipemia.
    • Kim GJ, Antonios Z, Knapper JME, Helen MR. Differences in glucose-dependent insulinotropic polypeptide hormone and hepatic lipase in subjects of southern and northern Europe: implications for postprandial lipemia. Am J Clin Nutr 2000; 71: 13-20.
    • (2000) Am J Clin Nutr , vol.71 , pp. 13-20
    • Kim, G.J.1    Antonios, Z.2    Knapper, J.M.E.3    Helen, M.R.4
  • 39
    • 34248223285 scopus 로고    scopus 로고
    • Biology of incretins: GLP-1 and GIP.
    • Baggio LL, Drucker DJ. Biology of incretins: GLP-1 and GIP. Gastroenterology 2007; 132: 2131-2157.
    • (2007) Gastroenterology , vol.132 , pp. 2131-2157
    • Baggio, L.L.1    Drucker, D.J.2
  • 40
    • 0027419106 scopus 로고
    • Additive insulinotropic effects of exogenous systemic human gastric inhibitory polypeptide and GLP-1(7-36) amide infused at near-physiological insulinotropic hormone and glucose concentration.
    • Nauck MA, Bartels E, Orskov C, Ebert R, Creutzfeldt W. Additive insulinotropic effects of exogenous systemic human gastric inhibitory polypeptide and GLP-1(7-36) amide infused at near-physiological insulinotropic hormone and glucose concentration. J Clin Endocrinol Metab 1993; 76: 912-917.
    • (1993) J Clin Endocrinol Metab , vol.76 , pp. 912-917
    • Nauck, M.A.1    Bartels, E.2    Orskov, C.3    Ebert, R.4    Creutzfeldt, W.5
  • 41
    • 0037299115 scopus 로고    scopus 로고
    • Effects of the novel (Pro3)GIP antagonist and exendin(9-39) amide on GIP- and GLP-1-induced cyclic AMP generation, insulin secretion and postprandial insulin release in obese diabetic (ob/ob) mice: evidence that GIP is the major physiological incretin.
    • Gault VA, O'Harte FPM, Harriott P. Effects of the novel (Pro3)GIP antagonist and exendin(9-39) amide on GIP- and GLP-1-induced cyclic AMP generation, insulin secretion and postprandial insulin release in obese diabetic (ob/ob) mice: evidence that GIP is the major physiological incretin. Diabetologia 2003; 46: 222-230.
    • (2003) Diabetologia , vol.46 , pp. 222-230
    • Gault, V.A.1    O'Harte, F.P.M.2    Harriott, P.3
  • 42
    • 12244270387 scopus 로고    scopus 로고
    • GIP as a potential therapeutic agent?
    • Meier JJ, Nauck MA. GIP as a potential therapeutic agent? Horm Metab Res 2004; 36: 859-866.
    • (2004) Horm Metab Res , vol.36 , pp. 859-866
    • Meier, J.J.1    Nauck, M.A.2


* 이 정보는 Elsevier사의 SCOPUS DB에서 KISTI가 분석하여 추출한 것입니다.