ライフサイエンスコーパス: glucagon receptor

1 recognition and transduction at the hepatic glucagon receptor.

2 nylate cyclase independent of binding to the glucagon receptor.

3 prise the primary ligand-binding site on the glucagon receptor.

4 different extramembrane segments of the rat glucagon receptor.

5 selectivity and G protein preference of the glucagon receptor.

6 se homeostasis through N-glycan branching on glucagon receptor.

7 ice with hepatocyte-specific deletion of the glucagon receptor.

8 on required for maximal interaction with the glucagon receptor.

9 ydrazones with modest affinity for the human glucagon receptor.

10 t changes in in vitro binding affinities for glucagon receptors.

11 genes including the parathyroid hormone and glucagon receptors.

12 pendent insulinotropic polypeptide (GIP) and glucagon receptors.

13 a multiple targets including GIP, GLP-1, and glucagon receptors.

14 receptor substrate-1, glycogen synthase, the glucagon receptor, a ras-related protein (Rad), histocom

15 hat the hepatic energy state is sensitive to glucagon receptor activation and requires PEPCK-C, thus

16 hypothesis that exercise-stimulated hepatic glucagon receptor activation is critical to reduce HFD-i

17 ng in hybrid peptides with potent dual GLP-1/glucagon receptor activity.

18 fects of G49, a dual glucagon-like peptide-1/glucagon receptor agonist, on NASH and hepatic regenerat

19 Dual-acting glucagon-like peptide-1/glucagon receptor agonists such as G49 represent a novel

20 ese hamster ovary cells expressing the human glucagon receptor and decreases the maximal glucagon sti

21 f skyrin on cells transfected with the human glucagon receptor and on isolated rat and human hepatocy

22 ctural and topographical requirements of the glucagon receptor, and, in addition, utilizing previous

23 A glucagon receptor antagonist (2-aminobenzimidazole) atte

24 A potent, selective glucagon receptor antagonist 9m, N-[(4-{(1S)-1-[3-(3,5-d

25 Finally, glucagon receptor antagonist improves glycemia in diet-i

26 r, these data suggest that Cpd 1 is a potent glucagon receptor antagonist that has the capability to

27 d plasma following an acute treatment with a glucagon receptor antagonist.

28 oning as both a GLP-1 receptor agonist and a glucagon receptor antagonist.

29 eration of progenitors in the CMZ, whereas a glucagon-receptor antagonist promoted proliferation.

30 on suppressed equatorial eye growth, whereas glucagon receptor antagonists caused excessive equatoria

31 Glucagon receptor antagonists have been developed as dru

32 eptidyl, triarylimidazole and triarylpyrrole glucagon receptor antagonists.

33 nstrated that these ligands were competitive glucagon receptor antagonists.

34 rotein-coupled fatty-acid-receptor agonists, glucagon-receptor antagonists, and metabolic inhibitors

35 ribes the antidiabetic effects of a specific glucagon receptor antisense oligonucleotide (GR-ASO) in

36 tail and the first extracellular loop of the glucagon receptor are required for hormone binding.

37 rs were increased by using glucagon, because glucagon receptors are predominantly on pericentral hepa

38 dback control gains of insulin receptors and glucagon receptors are robust.

39 This study reveals the glucagon receptor as a previously unidentified target fo

40 The antibodies bound specifically to native glucagon receptor as judged by immunofluorescence micros

41 gen in liver and the dynamics of insulin and glucagon receptors at the molecular level.

42 of retinal development, we detected mRNA for glucagon receptor beginning at E7 and mRNA for GLP1 rece

43 attempts to identify small molecular weight glucagon receptor-binding antagonists have met with litt

44 ds and their transport into alpha-cells link glucagon receptor blockage to alpha-cell hyperplasia.

45 Furthermore, administration of glucagon receptor-blocking antibody to healthy individua

46 y, mAb1, reveals that this antibody inhibits glucagon receptor by occluding a surface extending acros

47 est that at least three conformations of the glucagon receptor can exist in the membrane based on the

48 m at the glucagon-like peptide 1 (GLP-1) and glucagon receptors can restore leptin responsiveness in

49 udies support the concept that antagonism of glucagon receptors could be an effective approach for co

50 In CHO cells overexpressing the human glucagon receptor, Cpd 1 increased the half-maximal effe

51 ctural determinants of ligand binding in the glucagon receptor, eight receptor chimeras and additiona

52 Reducing glucagon receptor expression may thus ameliorate the con

53 istinct from but most closely related to the glucagon receptor family.

54 py to study receptor interactions within the glucagon receptor family.

55 Putative topographical requirements of the glucagon receptor for the aromatic side chain conformati

56 tional glucagon antagonism by uncoupling the glucagon receptor from adenylate cyclase activation in r

57 cate that functional uncoupling of the human glucagon receptor from cAMP production results in metabo

58 Thus, the glucagon receptor/G-protein/cAMP pathway regulates COX a

59 Recent studies report that mice lacking glucagon receptor (Gcgr(-/-)) do not develop diabetes fo

60 Mice genetically deficient in the glucagon receptor (Gcgr(-/-)) show improved glucose tole

61 We developed a novel stable and soluble glucagon receptor (GcgR) agonist, which allowed for in v

62 gon-like peptide-1 receptor (GLP-1R) and the glucagon receptor (GCGR) are members of the secretin-lik

63 emarkably, mice genetically deficient in the glucagon receptor (Gcgr) are refractory to the pathophys

64 Glucagon receptor (GcgR) blockade has been proposed as a

65 agon-like peptide 1 (GLP-1) receptor (GLP1R)/glucagon receptor (GCGR) dual agonist peptide that reduc

66 To elucidate the role of the hepatic glucagon receptor (Gcgr) in glucagon action, we generate

67 would reverse hyperglycemia, we targeted the glucagon receptor (GCGR) in rodent models of type 2 diab

68 Using this model, we show that glucagon receptor (GCGR) inhibition with a monoclonal an

69 evated glucagon levels and increased hepatic glucagon receptor (GCGR) signaling contribute to hypergl

70 Binding of the glucagon peptide to the glucagon receptor (GCGR) triggers the release of glucose

71 ECD and 7TM domain crystal structures of the glucagon receptor (GCGR), we examine the relationship be

72 transduced by the class B G-protein-coupled glucagon receptor (GCGR), which is located on liver, kid

73 ological functions through activation of the glucagon receptor (GCGR).

74 The human glucagon receptor, GCGR, belongs to the class B G-protei

75 fective (LepR(-/-)) rodents with and without glucagon receptors (GcgRs).

76 epends on enhanced signaling through hepatic glucagon receptors (GCGRs).

77 dered hypoglycemic by a null mutation in the glucagon receptor gene Gcgr display late-onset retinal d

78 dered hypoglycemic by a null mutation of the glucagon receptor gene, Gcgr.

79 ulin in the insulin receptor; insulin in the glucagon receptor; glucagon in the glucagon receptor; gl

80 in in the glucagon receptor; glucagon in the glucagon receptor; glucagon in the insulin receptor; and

81 We have recently cloned the murine glucagon receptor (GR) gene and shown that it is express

82 ional differences in the interactions of the glucagon receptor (GR) with the two predominant splice v

83 n of the glucagon-like peptide 1 (GLP-1) and glucagon receptor has the potential to lead to a novel t

84 e adverse side-effects, and targeting of the glucagon receptor has yet to be successful.

85 roimidazolone-based antagonists of the human glucagon receptor (hGCGR) has been developed.

86 ation of glucagon or genetic deletion of the glucagon receptor improved glucose homeostasis in animal

87 role of the COOH-terminal tail of the human glucagon receptor in glucagon-stimulated signal transduc

88 The mobility of glucagon receptor in primary hepatocytes was reduced by

89 ate manifestations of diabetes, we expressed glucagon receptors in livers of glucagon receptor-null (

90 Here we report the mechanisms of glucagon receptor inhibition by blocking antibodies targ

91 These data show that Angptl4 does not link glucagon receptor inhibition to compensatory hyperglucag

92 angiopoietin-like protein 4 (Angptl4) links glucagon receptor inhibition to hyperglucagonemia and al

93 The glucagon receptor is a member of a distinct class of G p

94 binding affinity of L-168,049 for the human glucagon receptor is decreased 24-fold by the inclusion

95 Antagonizing the glucagon receptor is expected to result in reduced hepat

96 that Angptl4(-/-) mice treated with an anti-glucagon receptor monoclonal antibody undergo elevation

97 db mice for 3 weeks resulted in 1) decreased glucagon receptor mRNA expression in liver; 2) decreased

98 The ability of GR-ASOs to inhibit glucagon receptor mRNA expression was demonstrated in pr

99 In transient transfection experiments, glucagon receptor mutants that bound glucagon but failed

100 To identify the components of the glucagon receptor necessary for G-protein coupling, we r

101 Glucagon receptor null (gcgr(-/-)) and wild-type (gcgr(+

102 ol mice, but these changes were abolished in glucagon receptor- null mice and mice with liver-specifi

103 rtinent clinical and metabolic parameters in glucagon receptor-null (Gcgr(-/-)) mice and wild-type (G

104 we expressed glucagon receptors in livers of glucagon receptor-null (GcgR(-/-)) mice before and after

105 High-fat-fed (HFF) glucagon receptor-null mice did not develop hyperinsulin

106 ficiency; (d) total beta cell destruction in glucagon receptor-null mice does not cause diabetes; and

107 subjects with inactivating mutations of the glucagon receptor, pancreatic swelling may be the first

108 omitant with increased hepatic expression of glucagon receptor, phosphorylated AMP-activated protein

109 ion of its own gene by signaling through the glucagon receptor, PKC, and PKA, supporting the more gen

110 , beta-adrenergic, histamine, serotonin, and glucagon receptors) play a key role in cardiac inotropy.

111 It is selective for glucagon receptor relative to other family B GPCRs, show

112 ative second intracellular loop of the human glucagon receptor results in a protein with high affinit

113 Glucagon receptor signaling and gluconeogenesis in Mgat5

114 Glucagon receptor signaling was hypothesized to mediate

115 to provide a more complete understanding of glucagon receptor signaling, considering the effect of m

116 show that the i2 and i3 loops play a role in glucagon receptor signaling, consistent with recent mode

117 l as to residues around its highly conserved glucagon receptor subfamily recognition fold.

118 eutically used GLP-1 receptor ligands at the glucagon receptor that is abolished by RAMP2 interaction

119 lization of the binding interaction with the glucagon receptor that leads to maximum biological poten

120 We demonstrate that the PPARalpha and glucagon receptors, the two instrumental transducers in

121 e prepared a stable cell line expressing the glucagon receptor to characterize the effect of G(s)-cou

122 timulated cAMP production in GIP, GLP-1, and glucagon receptor-transfected cells.

123 We found that the glucagon receptor was expressed by cells in the fibrous

124 93 cells, signaling by ectopically expressed glucagon receptor was increased by Mgat5 expression and

125 0-231 in the first extracellular loop of the glucagon receptor were replaced with the corresponding s

126 ral peptides that bind to both the GLP-1 and glucagon receptors were identified.

127 inding of 125I-labeled glucagon to the human glucagon receptor with a half-maximal inhibitory concent

128 its binding of labeled glucagon to the human glucagon receptor with an IC50 = 3.7 +/- 3.4 nM (n = 7)

129 uction in CHO cells overexpressing the human glucagon receptor with an IC50 of 3.4 nm.

130 lucagon analogues that can interact with the glucagon receptor with substantial binding affinity, 23

131 , i2, and i3) and the C-terminal tail of the glucagon receptor with the 11 amino acids comprising the

132 l and first extracellular loop domain of the glucagon receptor, with hormone specificity arising prim