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glucagon; contains: glicentin; glicentin-related polypeptide; GRPP; oxyntomodulin; OXM; OXY; glucagon-like peptide 1; GLP-1; glucagon-like peptide 1(7-37); GLP-1(7-37); glucagon-like peptide 1(7-36); GLP-1(7-36); glucagon-like peptide 2; GLP-2 (GCG)
Function:
- produced from cleavage of proglucagon
- role in glucose metabolism & homeostasis
- stimulates hepatic glycogenolysis & gluconeogenesis
- decreases glycolysis
- increases blood glucose levels
- counter-regulatory hormone of insulin, increases plasma glucose levels in response to insulin-induced hypoglycemia
- increases production of hepatic cAMP
- beta-adrenergic receptor agonist, positive inotropic & chronotropic activities
Structure:
- belongs to the glucagon family
- 54% of plasma glucagon activity is found in 160 kD component
- 9 & 3.5 kD components also show plasma glucagon activity
Compartment: secreted
Expression:
- glucagon is secreted by alpha cells of the pancreatic islets
- reciprocal relationship between plasma levels of glucagon & glucagon-like peptide-1 (GLP-1)
- GLP-1, GLP-2, oxyntomodulin & glicentin are secreted from enteroendocrine cells throughout the GI tract
- GLP-1 & GLP-2 are also secreted in selected neurons in the brain
- glucagon release is stimulated by hypoglycemia
- glucagon release isinhibited by hyperglycemia, insulin, & somatostatin
- GLP-1 & GLP-2 are induced in response to nutrient ingestion
Pathology:
- role in initiating & maintaining hyperglycemic conditions in diabetes mellitus
Pharmacology: see recombinant glucagon
Related
glucagon Ag in tissue
glucagon receptor; GL-R (GCGR)
glucose-6-phosphate dehydrogenase (G6PD) in tissue
Specific
enteroglucagon
Glucagon Parenteral
proglucagon
recombinant glucagon (Baqsimi)
General
endocrine agent
pancreatic hormone
secretin family peptide
Properties
SIZE: entity length = 180 aa
MW = 21 kD
COMPARTMENT: plasma
SECRETED-BY: alpha cell
WITHIN: islets of Langerhans
MOTIF: signal sequence {1-20}
proteolytic site {52-53}
proteolytic site {83-84}
proteolytic site {91-92}
proteolytic site {97-98}
proteolytic site {130-131}
proteolytic site {145-146}
MISC-INFO: elimination route LIVER
KIDNEY
CONCENTRATION 50-150 PG/ML
pregnancy-category B
safety in lactation ?
Database Correlations
OMIM 138030
UniProt P01275
Pfam PF00123
Entrez Gene 2641
Kegg hsa:2641
References
- The Pharmacological Basis of Therapeutics, 9th ed.
Gilman et al, eds. Permagon Press/McGraw Hill, 1996
- Drug Information & Medication Formulary, Veterans Affairs,
Central California Health Care System, 1st ed., Ravnan et al
eds, 1998