ライフサイエンスコーパス: glucagon receptor

1 on required for maximal interaction with the glucagon receptor.

2 ydrazones with modest affinity for the human glucagon receptor.

3 recognition and transduction at the hepatic glucagon receptor.

4 nylate cyclase independent of binding to the glucagon receptor.

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

6 different extramembrane segments of the rat glucagon receptor.

7 esign of allosteric modulators targeting the glucagon receptor.

8 way effecting the physiological roles of the glucagon receptor.

9 way effecting the physiological roles of the glucagon receptor.

10 ass B G-protein-coupled receptor (GPCR), the glucagon receptor.

11 selectivity and G protein preference of the glucagon receptor.

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

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

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

15 genes including the parathyroid hormone and glucagon receptors.

16 ic polypeptide, glucagon-like peptide 1, and glucagon receptors.

17 pic polypeptide, glucagon-like peptide 1 and glucagon receptors.

18 pendent insulinotropic polypeptide (GIP) and glucagon receptors.

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

20 For the glucagon receptor (a Class B GPCR) we observed enhanced

21 liver accumulation of an antibody targeting glucagon receptor, a protein profoundly expressed in tha

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

23 for a monoclonal antibody antagonist of the glucagon receptor (Ab-4) to maintain glucose homeostasis

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

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

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

27 However, glucagon receptor agonism [when balanced with an increti

28 ide is a glucagon-like peptide-1 (GLP-1) and glucagon receptor agonist that may improve kidney functi

29 adutide (Cota) is a lipidated dual GLP-1 and Glucagon receptor agonist that was investigated for the

30 id (LWPLGA) for sustained delivery GLP-1 and Glucagon receptor agonist with controlled burst release.

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

32 se-dependent insulinotropic polypeptide, and glucagon receptor agonists on endogenous glucagon secret

33 Glucagon receptor agonists show promise as components of

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

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

36 and safety of survodutide (a dual agonist of glucagon receptor and GLP-1 receptor) in persons with MA

37 mediated by paracrine signaling through the glucagon receptor and glucagon-like peptide 1 (GLP-1) re

38 Dual agonism of glucagon receptor and glucagon-like peptide-1 (GLP-1) re

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

40 ow that ARRDC4 coimmunoprecipitates with the glucagon receptor, and ARRDC4 expression is suppressed b

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

42 Thus, glucagon receptor antagonism (pharmacological or genetic

43 Glucagon receptor antagonism treatment, however, did not

44 A glucagon receptor antagonist (2-aminobenzimidazole) atte

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

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

47 2) the SGLT2i empagliflozin (25 mg), 3) the glucagon receptor antagonist LY2409021 (300 mg), or 4) t

48 These findings may have implications for glucagon receptor antagonist or agonist-based therapies.

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

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

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

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

53 Although glucagon receptor antagonists (GRAs) have great potentia

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

55 Glucagon receptor antagonists have been developed as dru

56 nstrated that these ligands were competitive glucagon receptor antagonists.

57 eptidyl, triarylimidazole and triarylpyrrole glucagon receptor antagonists.

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

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

60 -agonist synthetic peptides at the GLP-1 and glucagon receptor are in clinical development as potenti

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

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

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

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

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

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

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

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

69 gulation of Vgf and Gcg expression following glucagon receptor blockade.

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

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

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

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

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

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

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

77 The pharmacodynamics of ALT-801, a GLP-1/glucagon receptor dual agonist optimized for NASH and we

78 gests agonists may be more promising against glucagon receptor dysregulation in metabolic disorders.

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

80 Reducing glucagon receptor expression may thus ameliorate the con

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

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

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

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

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

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

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

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

89 The glucagon receptor (GCGR) activated by the peptide hormon

90 Long-term glucagon receptor (GCGR) agonism is associated with hype

91 As such, a better understanding of chronic glucagon receptor (GCGR) agonism is essential to identif

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

93 Several peptide dual agonists of the human glucagon receptor (GCGR) and the glucagon-like peptide-1

94 y of volagidemab, an antagonistic monoclonal glucagon receptor (GCGR) antibody, as an adjunct to insu

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

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

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

98 l loop exists, where inhibition of the liver glucagon receptor (GCGR) causes hyperaminoacidemia and p

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

100 cs simulations to access the dynamics of the glucagon receptor (GCGR) ECD in the presence of native-l

101 we found two rare homozygous variants in the glucagon receptor (GCGR) gene that cosegregated with the

102 Blockade of the glucagon receptor (GCGR) has been shown to improve glyce

103 Despite the importance of the glucagon receptor (GCGR) in disease and in pharmaceutica

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

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

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

107 Inhibition of the liver glucagon receptor (GCGR) results in elevated plasma amin

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

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

110 study the extracellular domain (ECD) of the glucagon receptor (GCGR), a class B family GPCR that con

111 he pancreatic hormone glucagon activates the glucagon receptor (GCGR), a class B seven-transmembrane

112 show that RAMP2 directly interacts with the glucagon receptor (GCGR), a Family B GPCR responsible fo

113 ulinotropic polypeptide receptor (GIPR), and glucagon receptor (GcgR), leveraging the sequence homolo

114 s characterized by reduced expression of the glucagon receptor (GCGR), PEPCK, and genes involved in a

115 s characterized by reduced expression of the glucagon receptor (GCGR), PEPCK, and genes involved in a

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

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

118 Here, using both genders of mouse islets and glucagon receptor (gcgr)-deficient zebrafish (Danio reri

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

120 e compared the structure and function of the glucagon receptor (GCGR; family B) with the beta(2) adre

121 retin effects, oxyntomodulin (OXM) activates glucagon receptors (GCGR) and glucagon-like peptide-1 re

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

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

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

125 homozygous for two missense variants in the glucagon receptor gene (GCGR).

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

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

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

129 in in the glucagon receptor; glucagon in the glucagon receptor; glucagon in the insulin receptor; and

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

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

132 ional structures of GPCRs such as GLP-1R and glucagon receptor has helped to drive the rational desig

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

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

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

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

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

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

139 ion of the GIP receptor in the brain and the glucagon receptor in the liver and adipose tissue functi

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

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

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

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

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

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

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

147 Utilizing whole-body glucagon receptor knockout (Gcgr(-/-)) mice and their wi

148 Here, we observed fewer glucagon receptor missense variants than expected, as we

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

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

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

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

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

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

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

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

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

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

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

160 beling of a BCN-lysine-encoded transmembrane glucagon receptor on live cells.

161 also enabled rapid bioorthogonal labeling of glucagon receptors on live cells in as little as 15 s.

162 We investigate the presence of insulin and glucagon receptors on the HepG2 cell membrane and demons

163 The glucagon receptor, one such G protein-coupled receptor,

164 by pharmacological antagonism of either the glucagon receptor or V1bR.

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

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

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

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

169 eptor agonists targeting the GLP-1, GIP, and glucagon receptors produce meaningful weight loss in peo

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

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

172 insulinotropic polypeptide (GIP), GLP-1, and glucagon receptors, showed clinically meaningful glucose

173 Glucagon receptor signaling and gluconeogenesis in Mgat5

174 metabolism, indicating a dispensable role of glucagon receptor signaling in maternal glucose homeosta

175 Glucagon receptor signaling was hypothesized to mediate

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

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

178 ought to determine the role of hepatic Gcgr (glucagon receptor) signaling in plasma cholesterol regul

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

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

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

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

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

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

185 losteric communication mechanisms within the glucagon receptor using molecular dynamics simulations o

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

187 93 cells, signaling by ectopically expressed glucagon receptor was increased by Mgat5 expression and

188 0-231 in the first extracellular loop of the glucagon receptor were replaced with the corresponding s

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

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

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

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

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

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

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