Glucagon chemistry

Glucagon-like peptide 1 abasis of a new class of treatment for type 2 diabetes. Journal of Medicinal Chemistry, 47, 4128 134 (b) Vahl, T.P. and D Alessio, D.A. (2004) Gut peptides in the treatment of diabetes mellitus. Expert Opinion on Investigational Drugs, 13, 177-188 (c) Meier, J.J. and Nauck, M.A. 

Wingrove, D.E., Amatruda, J. and Gunter, T.E. (1984) Glucagon effects on the membrane potential and calcium uptake rate of rat liver mitochondria. Journal of Biological Chemistry, 259 (15), 9390-9394. 

The existence of cAMP as a compound mediating the action of adrenaline and glucagon on glycogen phosphorylase was first recognized in 1956 by Sutherland.168169 However, for many years most biochemists regarded cAMP as a curiosity and the regulatory chemistry of phosphorylase as an unusual specialization. That view was altered drastically when cAMP was found to function as a second messenger in the action of over 20 different hormones. Phosphorylation by... 

Figure 16.13 Structures of glucagon and the digestive hormones, indicating their homologies. (Asterisk indicates amidation of C-terminal amino acid residue, which occurs with some gut hormones.) (Reproduced by permission from Tietz NW, Rinker AD, Henderson AT. Gastric, pancreatic, and intestinal function. In Tietz NW, ed. Textbook of Clinical Chemistry. Philadelphia WB Saunders, 1986, p. 1439.)...

Glucagon-like peptide 1 (GLPl) GLP-1 receptor 30- and 31-residue peptide amide differed by a C-terminal Gly Stimulate insulin secretion Solid-phase V -Fmoc chemistry... 

Glucagon Glucagon receptor 29-residue peptide Increase blood glucose level Solid-phase A -Boc chemistry... 

Its primary action is inhibiting the release of GH from the pituitary gland. Somatostatin al.so suppresses the release of both insulin and glucagon. It causes a decrease in both cAMP levels and adenylate cyclase activity. It also inhibits calcium ion influx into the pituitary cells and suppresses glucose-induced pancreatic insulin secretion by activating and deactivating potassium ion and calcium ion permeability, respcc-tively. The chemistry. SARs, and potential clinical applications have been reviewed.--- ... 

Chemistry, mechanism, and effects Glucagon is the product of the A cells of the endocrine pancreas. Like insulin, glucagon is a peptide but unlike insulin, glucagon acts on G protein-coupled receptors. Activation of glucagon receptors, which are located in heart, smooth muscle, and liver, stimulates adenylyl cyclase and increases intracellular cAMP. This results in increases in the heart rate and the force of contraction, increased hepatic glycogenolysis and gluconeogenesis and relaxation of smooth muscle. The smooth muscle effect is particularly marked in the gut. 

Chen, Q., Pinon, D. I., Miller, L. J., Dong, M. (2009). Molecular basis of glucagon-like peptide 1 docking to its intact receptor studied with carboxyl-terminal photolabile probes. Jewma/ of Biological Chemistry, 284(49), 34135—34144. http //dx.doi.org/10.1074/ jbc.M109.038109. 

Cascieri, M.A. et al. (1999) Characterization of a novel, non-peptidyl antagonist of the human glucagon receptor. The Journal of Biological Chemistry, 274, 8694—8697. 

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