메뉴 건너뛰기




Volumn 332, Issue 1, 2010, Pages 274-280

Pharmacological characterization of human incretin receptor missense variants

Author keywords

[No Author keywords available]

Indexed keywords

CYCLIC AMP; GASTRIC INHIBITORY POLYPEPTIDE; GLUCAGON LIKE PEPTIDE 1; GLUCAGON LIKE PEPTIDE 1 RECEPTOR; GLUCOSE DEPENDENT INSULINOTROPIC POLYPEPTIDE RECEPTOR; HORMONE RECEPTOR; MUTANT PROTEIN; UNCLASSIFIED DRUG;

EID: 73949123418     PISSN: 00223565     EISSN: 15210103     Source Type: Journal    
DOI: 10.1124/jpet.109.160531     Document Type: Article
Times cited : (71)

References (35)
  • 2
    • 45549092254 scopus 로고    scopus 로고
    • Pharmacological analysis of human D1 AND D2 dopamine receptor missense variants
    • Al-Fulaij MA, Ren Y, Beinborn M, and Kopin AS (2008) Pharmacological analysis of human D1 AND D2 dopamine receptor missense variants. J Mol Neurosci 34:211-223.
    • (2008) J Mol Neurosci , vol.34 , pp. 211-223
    • Al-Fulaij, M.A.1    Ren, Y.2    Beinborn, M.3    Kopin, A.S.4
  • 3
    • 0031781959 scopus 로고    scopus 로고
    • Discovery of amino acid variants in the human glucose-dependent insulinotropic polypeptide (GIP) receptor: The impact on the pancreatic beta cell responses and functional expression studies in Chinese hamster fibroblast cells
    • Almind K, Ambye L, Urhammer SA, Hansen T, Echwald SM, Holst JJ, Gromada J, Thorens B, and Pedersen O (1998) Discovery of amino acid variants in the human glucose-dependent insulinotropic polypeptide (GIP) receptor: the impact on the pancreatic beta cell responses and functional expression studies in Chinese hamster fibroblast cells. Diabetologia 41:1194-1198.
    • (1998) Diabetologia , vol.41 , pp. 1194-1198
    • Almind, K.1    Ambye, L.2    Urhammer, S.A.3    Hansen, T.4    Echwald, S.M.5    Holst, J.J.6    Gromada, J.7    Thorens, B.8    Pedersen, O.9
  • 4
    • 1342308287 scopus 로고    scopus 로고
    • Ligand function at constitutively active receptor mutants is affected by two distinct yet interacting mechanisms
    • Beinborn M, Ren Y, Bläker M, Chen C, and Kopin AS (2004) Ligand function at constitutively active receptor mutants is affected by two distinct yet interacting mechanisms. Mol Pharmacol 65:753-760.
    • (2004) Mol Pharmacol , vol.65 , pp. 753-760
    • Beinborn, M.1    Ren, Y.2    Bläker, M.3    Chen, C.4    Kopin, A.S.5
  • 5
    • 22044446844 scopus 로고    scopus 로고
    • A human glucagon-like peptide-1 receptor polymorphism results in reduced agonist responsiveness
    • Beinborn M, Worrall CI, McBride EW, and Kopin AS (2005) A human glucagon-like peptide-1 receptor polymorphism results in reduced agonist responsiveness. Regul Pept 130:1-6.
    • (2005) Regul Pept , vol.130 , pp. 1-6
    • Beinborn, M.1    Worrall, C.I.2    McBride, E.W.3    Kopin, A.S.4
  • 6
    • 66049138465 scopus 로고    scopus 로고
    • Membrane-tethered ligands are effective probes for exploring class B1 G proteincoupled receptor function
    • Fortin JP, Zhu Y, Choi C, Beinborn M, Nitabach MN, and Kopin AS (2009) Membrane-tethered ligands are effective probes for exploring class B1 G proteincoupled receptor function. Proc Natl Acad Sci U S A 106:8049-8054.
    • (2009) Proc Natl Acad Sci U S A , vol.106 , pp. 8049-8054
    • Fortin, J.P.1    Zhu, Y.2    Choi, C.3    Beinborn, M.4    Nitabach, M.N.5    Kopin, A.S.6
  • 8
    • 0028998560 scopus 로고
    • Mutational analysis of cysteine residues within the extracellular domains of the human vasoactive intestinal peptide (VIP) 1 receptor identifies seven mutants that are defective in VIP binding
    • Gaudin P, Couvineau A, Maoret JJ, Rouyer-Fessard C, and Laburthe M (1995) Mutational analysis of cysteine residues within the extracellular domains of the human vasoactive intestinal peptide (VIP) 1 receptor identifies seven mutants that are defective in VIP binding. Biochem Biophys Res Commun 211:901-908.
    • (1995) Biochem Biophys Res Commun , vol.211 , pp. 901-908
    • Gaudin, P.1    Couvineau, A.2    Maoret, J.J.3    Rouyer-Fessard, C.4    Laburthe, M.5
  • 9
    • 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, and Flatt PR (2007) 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 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
  • 10
    • 0031018485 scopus 로고    scopus 로고
    • Structural instability of a constitutively active G protein-coupled receptor. Agonist-independent activation due to conformational flexibility
    • Gether U, Ballesteros JA, Seifert R, Sanders-Bush E, Weinstein H, and Kobilka BK (1997) Structural instability of a constitutively active G protein-coupled receptor. Agonist-independent activation due to conformational flexibility. J Biol Chem 272:2587-2590.
    • (1997) J Biol Chem , vol.272 , pp. 2587-2590
    • Gether, U.1    Ballesteros, J.A.2    Seifert, R.3    Sanders-Bush, E.4    Weinstein, H.5    Kobilka, B.K.6
  • 11
    • 16244383540 scopus 로고    scopus 로고
    • Mechanisms of peptide and nonpeptide ligand binding to Class B G-protein-coupled receptors
    • Hoare SR (2005) Mechanisms of peptide and nonpeptide ligand binding to Class B G-protein-coupled receptors. Drug Discov Today 10:417-427.
    • (2005) Drug Discov Today , vol.10 , pp. 417-427
    • Hoare, S.R.1
  • 12
    • 42449157201 scopus 로고    scopus 로고
    • Allosteric ligands for the corticotropin releasing factor type 1 receptor modulate conformational states involved in receptor activation
    • Hoare SR, Fleck BA, Gross RS, Crowe PD, Williams JP, and Grigoriadis DE (2008) Allosteric ligands for the corticotropin releasing factor type 1 receptor modulate conformational states involved in receptor activation. Mol Pharmacol 73:1371-1380.
    • (2008) Mol Pharmacol , vol.73 , pp. 1371-1380
    • Hoare, S.R.1    Fleck, B.A.2    Gross, R.S.3    Crowe, P.D.4    Williams, J.P.5    Grigoriadis, D.E.6
  • 15
    • 1942517868 scopus 로고    scopus 로고
    • Principles: Receptor theory in pharmacology
    • Kenakin T (2004) Principles: receptor theory in pharmacology. Trends Pharmacol Sci 25:186-192.
    • (2004) Trends Pharmacol Sci , vol.25 , pp. 186-192
    • Kenakin, T.1
  • 16
    • 20444491588 scopus 로고    scopus 로고
    • Glucosedependent insulinotropic polypeptide (GIP) stimulation of pancreatic beta-cell survival is dependent upon phosphatidylinositol 3-kinase (PI3K)/protein kinase B (PKB) signaling, inactivation of the forkhead transcription factor Foxo1, and down-regulation of bax expression
    • Kim SJ, Winter K, Nian C, Tsuneoka M, Koda Y, and McIntosh CH (2005) Glucosedependent insulinotropic polypeptide (GIP) stimulation of pancreatic beta-cell survival is dependent upon phosphatidylinositol 3-kinase (PI3K)/protein kinase B (PKB) signaling, inactivation of the forkhead transcription factor Foxo1, and down-regulation of bax expression. J Biol Chem 280:22297-22307.
    • (2005) J Biol Chem , vol.280 , pp. 22297-22307
    • Kim, S.J.1    Winter, K.2    Nian, C.3    Tsuneoka, M.4    Koda, Y.5    McIntosh, C.H.6
  • 17
    • 58149090676 scopus 로고    scopus 로고
    • The role of incretins in glucose homeostasis and diabetes treatment
    • KimWand Egan JM (2008) The role of incretins in glucose homeostasis and diabetes treatment. Pharmacol Rev 60:470-512.
    • (2008) Pharmacol Rev , vol.60 , pp. 470-512
    • KimWand Egan, J.M.1
  • 18
    • 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 A, Yamada Y, Hayami T, Yasuda K, Someya Y, Ihara Y, Kagimoto S, Watanabe R, Taminato T, Tsuda K, et al. (1996) 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 45:1701-1705.
    • (1996) Diabetes , vol.45 , pp. 1701-1705
    • Kubota, A.1    Yamada, Y.2    Hayami, T.3    Yasuda, K.4    Someya, Y.5    Ihara, Y.6    Kagimoto, S.7    Watanabe, R.8    Taminato, T.9    Tsuda, K.10
  • 20
    • 0027297275 scopus 로고
    • Constitutive activity of receptors coupled to guanine nucleotide regulatory proteins
    • Lefkowitz RJ, Cotecchia S, Samama P and Costa T (1993) Constitutive activity of receptors coupled to guanine nucleotide regulatory proteins. Trends Pharmacol Sci 14:303-307.
    • (1993) Trends Pharmacol Sci , vol.14 , pp. 303-307
    • Lefkowitz, R.J.1    Cotecchia, S.2    Samama, P.3    Costa, T.4
  • 21
    • 16844366813 scopus 로고    scopus 로고
    • Paired cysteine mutagenesis to establish the pattern of disulfide bonds in the functional intact secretin receptor
    • Lisenbee CS, Dong M, and Miller LJ (2005) Paired cysteine mutagenesis to establish the pattern of disulfide bonds in the functional intact secretin receptor. J Biol Chem 280:12330-12338.
    • (2005) J Biol Chem , vol.280 , pp. 12330-12338
    • Lisenbee, C.S.1    Dong, M.2    Miller, L.J.3
  • 22
    • 34548093246 scopus 로고    scopus 로고
    • Four missense mutations in the ghrelin receptor result in distinct pharmacological abnormalities
    • Liu G, Fortin JP, Beinborn M, and Kopin AS (2007) Four missense mutations in the ghrelin receptor result in distinct pharmacological abnormalities. J Pharmacol Exp Ther 322:1036-1043.
    • (2007) J Pharmacol Exp Ther , vol.322 , pp. 1036-1043
    • Liu, G.1    Fortin, J.P.2    Beinborn, M.3    Kopin, A.S.4
  • 23
    • 67651173077 scopus 로고    scopus 로고
    • Incretin-based therapies for type 2 diabetes mellitus
    • Lovshin JA and Drucker DJ (2009) Incretin-based therapies for type 2 diabetes mellitus. Nat Rev Endocrinol 5:262-269.
    • (2009) Nat Rev Endocrinol , vol.5 , pp. 262-269
    • Lovshin, J.A.1    Drucker, D.J.2
  • 24
    • 0242500960 scopus 로고    scopus 로고
    • Structure-function analysis of a series of novel GIP analogues containing different helical length linkers
    • Manhart S, Hinke SA, McIntosh CH, Pederson RA, and Demuth HU (2003) Structure-function analysis of a series of novel GIP analogues containing different helical length linkers. Biochemistry 42:3081-3088.
    • (2003) Biochemistry , vol.42 , pp. 3081-3088
    • Manhart, S.1    Hinke, S.A.2    McIntosh, C.H.3    Pederson, R.A.4    Demuth, H.U.5
  • 25
    • 0030990139 scopus 로고    scopus 로고
    • Scanning of the glucagon-like peptide-1 receptor localizes G protein-activating determinants primarily to the N terminus of the third intracellular loop
    • Mathi SK, Chan Y, Li X, and Wheeler MB (1997) Scanning of the glucagon-like peptide-1 receptor localizes G protein-activating determinants primarily to the N terminus of the third intracellular loop. Mol Endocrinol 11:424-432.
    • (1997) Mol Endocrinol , vol.11 , pp. 424-432
    • Mathi, S.K.1    Chan, Y.2    Li, X.3    Wheeler, M.B.4
  • 28
    • 0030820210 scopus 로고    scopus 로고
    • Extracellular cysteines of the corticotropin-releasing factor receptor are critical for ligand interaction
    • Qi LJ, Leung AT, Xiong Y, Marx KA, and Abou-Samra AB (1997) Extracellular cysteines of the corticotropin-releasing factor receptor are critical for ligand interaction. Biochemistry 36:12442-12448.
    • (1997) Biochemistry , vol.36 , pp. 12442-12448
    • Qi, L.J.1    Leung, A.T.2    Xiong, Y.3    Marx, K.A.4    Abou-Samra, A.B.5
  • 29
    • 45549086826 scopus 로고    scopus 로고
    • Crystal structure of the ligand-bound glucagon-like peptide-1 receptor extracellular domain
    • Runge S, Thøgersen H, Madsen K, Lau J, and Rudolph R (2008) Crystal structure of the ligand-bound glucagon-like peptide-1 receptor extracellular domain. J Biol Chem 283:11340-11347.
    • (2008) J Biol Chem , vol.283 , pp. 11340-11347
    • Runge, S.1    Thøgersen, H.2    Madsen, K.3    Lau, J.4    Rudolph, R.5
  • 30
    • 0031031054 scopus 로고    scopus 로고
    • Ligandinduced overexpression of a constitutively active beta2-adrenergic receptor: Pharmacological creation of a phenotype in transgenic mice
    • Samama P, Bond RA, Rockman HA, Milano CA, and Lefkowitz RJ (1997) Ligandinduced overexpression of a constitutively active beta2-adrenergic receptor: pharmacological creation of a phenotype in transgenic mice. Proc Natl Acad Sci U S A 94:137-141.
    • (1997) Proc Natl Acad Sci U S A , vol.94 , pp. 137-141
    • Samama, P.1    Bond, R.A.2    Rockman, H.A.3    Milano, C.A.4    Lefkowitz, R.J.5
  • 31
    • 0036033424 scopus 로고    scopus 로고
    • Constitutive activity of G-protein-coupled receptors: Cause of disease and common property of wild-type receptors
    • Seifert R and Wenzel-Seifert K (2002) Constitutive activity of G-protein-coupled receptors: cause of disease and common property of wild-type receptors. Naunyn Schmiedebergs Arch Pharmacol 366:381-416.
    • (2002) Naunyn Schmiedebergs Arch Pharmacol , vol.366 , pp. 381-416
    • Seifert, R.1    Wenzel-Seifert, K.2
  • 32
    • 0037387146 scopus 로고    scopus 로고
    • Regulation of melanocortin-4 receptor signaling: Agonist-mediated desensitization and internalization
    • Shinyama H, Masuzaki H, Fang H, and Flier JS (2003) Regulation of melanocortin-4 receptor signaling: agonist-mediated desensitization and internalization. Endocrinology 144:1301-1314.
    • (2003) Endocrinology , vol.144 , pp. 1301-1314
    • Shinyama, H.1    Masuzaki, H.2    Fang, H.3    Flier, J.S.4
  • 33
    • 0035851103 scopus 로고    scopus 로고
    • A small molecule ligand of the glucagon-like peptide 1 receptor targets its amino-terminal hormone binding domain
    • Tibaduiza EC, Chen C, and Beinborn M (2001) A small molecule ligand of the glucagon-like peptide 1 receptor targets its amino-terminal hormone binding domain. J Biol Chem 276:37787-37793.
    • (2001) J Biol Chem , vol.276 , pp. 37787-37793
    • Tibaduiza, E.C.1    Chen, C.2    Beinborn, M.3
  • 34
    • 0031555863 scopus 로고    scopus 로고
    • A point mutation in the glucose-dependent insulinotropic peptide receptor confers constitutive activity
    • Tseng CC and Lin L (1997) A point mutation in the glucose-dependent insulinotropic peptide receptor confers constitutive activity. Biochem Biophys Res Commun 232: 96-100.
    • (1997) Biochem Biophys Res Commun , vol.232 , pp. 96-100
    • Tseng, C.C.1    Lin, L.2
  • 35
    • 0033927916 scopus 로고    scopus 로고
    • Melanocortin-4 receptor mutations are a frequent and heterogeneous cause of morbid obesity
    • Vaisse C, Clement K, Durand E, Hercberg S, Guy-Grand B, and Froguel P (2000) Melanocortin-4 receptor mutations are a frequent and heterogeneous cause of morbid obesity. J Clin Invest 106:253-262.
    • (2000) J Clin Invest , vol.106 , pp. 253-262
    • Vaisse, C.1    Clement, K.2    Durand, E.3    Hercberg, S.4    Guy-Grand, B.5    Froguel, P.6


* 이 정보는 Elsevier사의 SCOPUS DB에서 KISTI가 분석하여 추출한 것입니다.