Biology of Incretins: GLP-1 and GIP
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Cites background or methods from "Biology of Incretins: GLP-1 and GIP..."
...Background—The glucagon-like peptide 1 receptor (GLP-1R) is believed to mediate glucoregulatory and cardiovascular effects of the incretin hormone GLP-1(7-36) (GLP-1), which is rapidly degraded by dipeptidyl peptidase-4 (DPP-4) to GLP-1(9-36), a truncated metabolite generally thought to be inactive....
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...4,5 After secretion from enteroendocrine L cells, GLP-1(7-36) amide is rapidly degraded by dipeptidyl peptidase-4 (DPP-4) to its N-terminally truncated metabolite GLP-1(9-36), which does not interact with the known GLP-1 receptor....
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...2,3 Active isoforms of GLP-1 include GLP-1(7-36) amide and glycine-extended GLP-1(7-37)....
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...GLP-1(7-36) by DPP-4–mediated cleavage, might be respon-...
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...Studies using a DPP-4–resistant GLP-1R agonist and inhibitors of DPP-4 and nitric oxide synthase showed that the effects of GLP-1(7-36) were partly mediated by GLP-1(9-36) through a nitric oxide synthase–requiring mechanism that is independent of the known GLP-1R....
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Cites background from "Biology of Incretins: GLP-1 and GIP..."
...The primary physiological stimuli for the secretion of GLP-1 are fat- and carbohydrate-rich meals, but mixed meals or individual nutrients, including glucose and other sugars, sweeteners, fatty acids, amino acids, and dietary fiber, also can stimulate GLP-1 secretion (Baggio and Drucker, 2007)....
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...The degree to which nutrients regulate GIP secretion is species-dependent because fat is a more potent stimulator of GIP secretion than carbohydrates in humans, whereas, in the rodent and pig, carbohydrates are more potent than fat (Baggio and Drucker, 2007)....
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...Specific serine residues within the CT, particularly serines 426 and 427, play an important role in regulating the rate of receptor internalization, whereas serines 406 and 411 are important for receptor desensitization (Wheeler et al., 1999; Baggio and Drucker, 2007)....
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...Although the majority of the cytoplasmic domain of the GIPR mediates intracellular signal transduction, a minimum length of approximately 405 amino acids is required for efficient transport and plasma membrane insertion (Baggio and Drucker, 2007)....
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References
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