The effects of species ortholog and SNP variation on receptors for free fatty acids [PDF]
, 2013 Although it is widely assumed that species orthologs of hormone responsive G protein-coupled receptors will be activated by the same endogenously produced ligand(s), variation in potency, particularly in cases where more than one receptor responds to the
1000 Genomes Project Consortium +72 more
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Journal of Diabetes Investigation, 2019 Aims/Introduction Tofogliflozin is a potent and highly selective sodium–glucose cotransporter 2 inhibitor that is currently used to treat patients with type 2 diabetes mellitus.
Yasuo Terauchi +7 more
doaj +1 more source
The therapeutic potential of allosteric ligands for free fatty acid sensitive GPCRs [PDF]
, 2013 G protein coupled receptors (GPCRs) are the most historically successful therapeutic targets. Despite this success there are many important aspects of GPCR pharmacology and function that have yet to be exploited to their full therapeutic potential.
Hudson, Brian D. +2 more
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What doesn't kill you makes you stranger: Dipeptidyl peptidase-4 (CD26) proteolysis differentially modulates the activity of many peptide hormones and cytokines generating novel cryptic bioactive ligands [PDF]
, 2019 Dipeptidyl peptidase 4 (DPP4) is an exopeptidase found either on cell surfaces where it is highly regulated in terms of its expression and surface availability (CD26) or in a free/circulating soluble constitutively available and intrinsically active form.
Aguilar-Pérez, Alexandra +13 more
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Molecular Metabolism, 2021 Objective: We assessed the spatiotemporal GLP-1 and GIP receptor signaling, trafficking, and recycling dynamics of GIPR mono-agonists, GLP-1R mono-agonists including semaglutide, and GLP-1/GIP dual-agonists MAR709 and tirzepatide.
Aaron Novikoff +13 more
doaj +1 more source
The effect of the GLP-1 analogue Exenatide on functional connectivity within an NTS-based network in women with and without obesity. [PDF]
, 2017 ObjectiveThe differential effect of GLP-1 agonist Exenatide on functional connectivity of the nucleus tractus solitaries (NTS), a key region associated with homeostasis, and on appetite-related behaviours was investigated in women with normal weight ...
Connolly, L +7 more
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In-Silico Design of Novel Glucagon-Like Peptide 1 Mutants as Candidate for New Peptide Agonist Drugs
Hayati Journal of Biosciences, 2021 The binding of glucagon-like peptide 1 (GLP-1) incretin hormone and its receptor GLP-1R plays an important role in the human body. The GLP-1 acts as the insulin secretion stimulator through a GLP-1R agonist activation to avoid the type 2 diabetes ...
Tony Sumaryada +4 more
doaj
Allosteric modulation of the activity of the glucagon-like peptide-1 (GLP-1) metabolite GLP-1 9-36 amide at the GLP-1 receptor. [PDF]
PLoS ONE, 2012 Glucagon-like peptide-1 (GLP-1) released from intestinal L cells in response to nutrients has many physiological effects but particularly enhances glucose-dependent insulin release through the GLP-1 receptor (GLP-1R).
Naichang Li, Jing Lu, Gary B Willars
doaj +1 more source
Value of the radiolabelled GLP-1 receptor antagonist exendin(9-39) for targeting of GLP-1 receptor-expressing pancreatic tissues in mice and humans [PDF]
, 2018 Purpose: Radiolabelled glucagon-like peptide 1 (GLP-1) receptor agonists have recently been shown to successfully image benign insulinomas in patients.
Reubi, Jean, Waser, Beatrice
core
Continued efforts to translate diabetes cardiovascular outcome trials into clinical practice [PDF]
, 2016 Diabetic patients suffer from a high rate of cardiovascular events and such risk increases with HbA1c. However, lowering HbA1c does not appear to yield the same benefit on macrovascular endpoints, as observed for microvascular endpoints. As the number of
Avogaro, Angelo +4 more
core +3 more sources