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Biology of incretins: GLP-1 and GIP.
This review focuses on the mechanisms regulating the synthesis, secretion, biological actions, and therapeutic relevance of the incretin peptides glucose-dependent insulinotropic polypeptide (GIP)Expand
The incretin system: glucagon-like peptide-1 receptor agonists and dipeptidyl peptidase-4 inhibitors in type 2 diabetes
Clinical trials with the incretin mimetic exenatide and liraglutide show reductions in fasting and postprandial glucose concentrations, and haemoglobin A1c (HbA1c) associated with weight loss, but long-term clinical studies are needed to determine the benefits of targeting the inc retin axis for the treatment of type 2 diabetes. Expand
The biology of incretin hormones.
  • D. Drucker
  • Biology, Medicine
  • Cell metabolism
  • 1 March 2006
Current concepts of incretin action are summarized and the potential therapeutic utility of GLP-1 receptor agonists and dipeptidyl peptidase-4 (DPP-4) inhibitors for the treatment of type 2 diabetes is highlighted. Expand
Cardioprotective and Vasodilatory Actions of Glucagon-Like Peptide 1 Receptor Are Mediated Through Both Glucagon-Like Peptide 1 Receptor–Dependent and –Independent Pathways
It is shown that endothelium and cardiac and vascular myocytes express a functional GLP-1R as GLp-1 administration increased glucose uptake, cAMP and cGMP release, left ventricular developed pressure, and coronary flow in isolated mouse hearts, and this data suggest that the extent to which GLP -1 is metabolized to GLP(9-36) may have functional implications in the cardiovascular system. Expand
Exenatide once weekly versus twice daily for the treatment of type 2 diabetes: a randomised, open-label, non-inferiority study
Exen atide once weekly resulted in significantly greater improvements in glycaemic control than exenatide given twice a day, with no increased risk of hypoglycaemia and similar reductions in bodyweight. Expand
Pharmacology, physiology, and mechanisms of incretin hormone action.
Whether mechanisms identified in preclinical studies have potential translational relevance for the treatment of human disease and highlight controversies and uncertainties in incretin biology that require resolution in future studies are discussed. Expand
FTO Obesity Variant Circuitry and Adipocyte Browning in Humans.
The data indicate that the FTO allele associated with obesity represses mitochondrial thermogenesis in adipocyte precursor cells in a tissue-autonomous manner, and points to a pathway for adipocyte thermogenesis regulation involving ARID5B, rs1421085, IRX3, and IRX5, which, when manipulated, had pronounced pro-obesity and anti-ob obesity effects. Expand
Enhancing incretin action for the treatment of type 2 diabetes.
The need for daily injections of potentially immunogenic GLP-1-derived peptides and the potential for unanticipated side effects with chronic use of DPP-IV inhibitors will require ongoing scrutiny of the risk-benefit ratio for these new therapies as they are evaluated in the clinic. Expand
Glucagon-like peptide-1 receptor is involved in learning and neuroprotection
Systemic administration of [Ser(2)]exendin(1–9) in wild-type animals prevents kainate-induced apoptosis of hippocampal neurons and represents a promising new target for both cognitive-enhancing and neuroprotective agents. Expand
Glucagon-like peptide I stimulates insulin gene expression and increases cyclic AMP levels in a rat islet cell line.
It is reported that the smaller of the two glucagon-like peptides potently increases cAMP levels, insulin mRNA transcripts, and insulin release in cultured rat insulinoma cells, indicating that glucagon -like peptide I may be a physiologic modulator of insulin gene expression. Expand