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What is this compound we're working with

GLP-1 Key Research Facts Full name: Glucagon-Like Peptide-1 incretin hormone of the proglucagon family Primary bioactive form: GLP-1(736)amide 30 amino acids, C-terminally amidated Gene source: Proglucagon gene processed by PCSK1 in intestinal L-cells and brainstem NTS neurons In vivo half-life: Approximately 12 minutes rapidly inactivated by DPP-4 (cleaves His7-Ala8 dipeptide) Primary receptor: GLP-1R (GLP-1 receptor) class B G protein-coupled receptor (GPCR) Signalling: GLP-1R activation cAMP elevation PKA/CREB activation glucose-dependent insulin secretion Additional signalling: PI3K/Akt pathway -cell survival, proliferation, and glucose sensitivity Secretion pattern: Biphasic post-meal release from intestinal L-cells early neural/endocrine peak + late direct nutrient-contact peak Fasting plasma level: ~510 pmol/L

Kamenicky, P., Mazziotti, G., Lombes, M., Giustina, A

Mechanisms of apoptosis sensitivity and resistance to the BH3 mimetic ABT-737 in acute myeloid leukemia

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