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A novel glucagon receptor antagonist inhibits glucagon-mediated biological effects

- diabetesjournals.org
SA Qureshi, R Candelore… - Diabetes, 2004 - Am Diabetes Assoc
Glucagon maintains glucose homeostasis during the fasting state by promoting
hepatic gluconeogenesis and glycogenolysis. Hyperglucagonemia and/or an elevated
glucagon-to-insulin ratio have been reported in diabetic patients and ...
Cited by 18 - Related articles - BL Direct - All 5 versions

Reduction in glucagon receptor expression by an antisense oligonucleotide ameliorates …


Y Liang, MC Osborne, BP Monia, S Bhanot, … - Diabetes, 2004 - Am Diabetes Assoc
Excess glucagon levels contribute to the hyperglycemia associated with type 2
diabetes. Reducing glucagon receptor expression may thus ameliorate the
consequences of hyperglucagonemia and improve blood glucose control in ...
Cited by 47 - Related articles - BL Direct - All 5 versions

Hepatic glucagon receptor binding and glucose-lowering in vivo by peptidyl and non- …


Q Dallas-Yang, X Shen, M Strowski, E Brady, … - European journal of pharmacology, 2004 - Elsevier
Glucagon receptor antagonists have been actively pursued as potential
therapeutics for the treatment of type 2 diabetes. Peptidyl and non-peptidyl
glucagon receptor antagonists have been shown to block glucagon-induced ...
Cited by 8 - Related articles - All 3 versions

Hepatic and glucagon-like peptide-1–mediated reversal of diabetes by glucagon receptor …

- nih.gov
KW Sloop, JXC Cao, AM Siesky, HY Zhang, DM … - Journal of Clinical Investigation, 2004 - Am Soc Clin Investig
Uncontrolled hepatic glucose production contributes significantly to
hyperglycemia in patients with type 2 diabetes. Hyperglucagonemia is implicated
in the etiology of this condition; however, effective therapies to block ...
Cited by 47 - Related articles - BL Direct - All 6 versions

Immunoneutralization of endogenous glucagon reduces hepatic glucose output and improves …


H Sørensen, CL Brand, S Neschen, JJ Holst, … - Diabetes, 2006 - Am Diabetes Assoc
In type 2 diabetes, glucagon levels are elevated in relation to the prevailing
insulin and glucose levels. The relative hyperglucagonemia is linked to
increased hepatic glucose output (HGO) and hyperglycemia. Antagonizing the ...
Cited by 14 - Related articles - BL Direct - All 6 versions

Discovery of novel, potent, and orally active spiro-urea human glucagon receptor …


DM Shen, F Zhang, EJ Brady, MR Candelore, … - Bioorganic & Medicinal Chemistry Letters, 2005 - Elsevier
AM1 computer modeling of compound 1 with the three peripheral substituents
truncated for ease of computation showed conformers A and B to have very similar
energies. 12 A quick visual inspection revealed that a slightly lower ...
Cited by 6 - Related articles - All 4 versions

Human glucagon receptor antagonists based on alkylidene hydrazides


A Ling, M Plewe, J Gonzalez, P Madsen, CK … - Bioorganic & Medicinal Chemistry Letters, 2002 - Elsevier
Previously we reported the discovery of a class of human glucagon receptor
antagonists exemplified by 3-chloro-4-hydroxybenzoic acid (4-hydroxy-1-
naphthylmethylene)hydrazide (1) prepared from the condensation of ...
Cited by 17 - Related articles - BL Direct - All 4 versions

Effects of a novel glucagon receptor antagonist (Bay 27–9955) on glucagon-stimulated …


KF Petersen, JT Sullivan - Diabetologia, 2001 - Springer
Fasting hyperglycaemia in patients with poorly con- trolled Type II
(non-insulin-dependent) diabetes mellitus is closely associated with increased
rates of glucose production which in turn can be ascribed to increased ...
Cited by 62 - Related articles - BL Direct - All 3 versions

Glycemic control in mice with targeted disruption of the glucagon receptor gene


JC Parker, KM Andrews, MR Allen, JL Stock, … - Biochemical and Biophysical Research …, 2002 - Elsevier
The action of glucagon in the liver is mediated by G-coupled receptors. To
examine the role of glucagon in glucose homeostasis, we have generated mice in
which the glucagon receptor was inactivated (GR −/− mice). Blood ...
Cited by 44 - Related articles - BL Direct - All 6 versions

Glucagon as a target for the treatment of type 2 diabetes


KW Sloop, MD Michael, JS Moyers - Expert Opin. Ther. Targets, 2005 - informahealthcare.com
Glucagon is the key counter-regulatory hormone that opposes the action of
insulin. In states of relative hypoglycaemia, glucagon acts to increase blood
glucose by stimulating hepatic glycogen breakdown and gluconeogenesis to ...
Cited by 12 - Related articles - BL Direct - All 4 versions


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