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Incretin

También conocido como: GIP, GLP-1, incretin hormone

Incretins are gut-derived hormones — principally GIP and GLP-1 — that potentiate glucose-dependent insulin signaling. Synthetic incretin-receptor agonists are studied in vitro for receptor binding and downstream cAMP signaling.

Incretins are released by enteroendocrine cells of the gut in response to nutrients — GIP from K cells and GLP-1 from L cells — and the term reflects the observation that oral glucose provokes a larger insulin response than an equivalent intravenous load. Both hormones act on class B G protein-coupled receptors, GIPR and GLP-1R, through the Gs/cAMP pathway.

Native incretins are inactivated within minutes by the protease DPP-4, so engineered research analogs incorporate modifications that resist this cleavage.

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