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Therapy of acute myocardial infarction
Published in Wilbert S. Aronow, Jerome L. Fleg, Michael W. Rich, Tresch and Aronow’s Cardiovascular Disease in the Elderly, 2019
Joshua M. Stolker, Michael W. Rich
The glucagon-like peptide-1 receptor (GLP-1) agonists, another newer class of diabetes therapies, has demonstrated more variable outcomes in randomized trials, with several trials demonstrating cardiovascular safety but not superiority to existing diabetes or cardiac therapies. However, liraglutide reduced the primary composite endpoint of cardiovascular death, MI, or stroke by 13% (1.9% absolute reduction) among 9340 patients with type 2 diabetes and prevalent cardiovascular disease—approximately 30% of whom had prior MI (122). Patients with prior coronary events appeared to gain the most benefit during the median 3.8 years of follow-up, but unlike the SGLT2 inhibitor trials, older patients experienced less benefit in subgroup analyses. Gastrointestinal distress was the primary adverse event with liraglutide, and subcutaneous administration is required. As such, the role of GLP-1 agonists in this population remains to be determined.
Marine Bioactive Compounds: Innovative Trends in Food and Medicine
Published in Megh R. Goyal, Durgesh Nandini Chauhan, Plant- and Marine-Based Phytochemicals for Human Health, 2018
Munawar Abbas, Farhan Saeed, Hafiz Ansar Rasul Suleria
Cardiovascular disease (CVD) is a major disorder that affects blood vessels and heart causing heart failure, cerebrovascular disease (stroke), peripheral vascular disease, heart disease (heart attack), and hypertension (high blood pressure).48 In 1999, only CVD contributed to about 1/3 of world deaths and, in 2010, it will be major reason of death in the developing countries.84 Researches have revealed the preventive role of high fruitsand vegetable diet against CVD.27, 84 In addition, ω-3 PUFAs, antioxidants, vitamins and minerals, and dietary fibers with physical exercise are important to control and cure CVD. The risk of CVD can be lowered by glucose-lowering agents. Glucagon-like peptide-1 receptor (GLP-1R) belongs to B1 family of G protein, a paired receptor36 and has been found to lower blood sugar level. Control of heart rate and blood pressure is very complex and is species specific due to GLP-1.
Protecting Pancreatic β-cells from Metabolic Insults
Published in Christophe Wiart, Medicinal Plants in Asia for Metabolic Syndrome, 2017
Geniposide from the fruits of Gardenia jasminoides J. Ellis at a concentration of 10 µmol/L induced the secretion of insulin in vitro by INS-1 rat insulinoma cell line to about 10 ng/mL/h and this effect was dose dependent.317 This iridoid glucoside at 10 µmol/L potentiated insulin secretion evoked by glucose and this effect was abrogated by glucagon-like peptide-1 receptor antagonist exendin.318 Geniposide (Figure 2.21) at a concentration of 10 µM protected INS-1 rat insulinoma cells against palmitic acid-induced apoptosis.317 This effect was abolished by glucagon-like peptide-1 receptor antagonist exendin.318 Geniposide increased the level of pancreatic and duodenal homeobox-1, and reversed palmitate-induced decreased phosphorylation of Akt, and Foxo1.318 Note that geniposide is decomposed into genipin by bacterial flora (Aburada et al., 1978) hence a probable lower ability to be as effective orally.319
Evolution of phage display libraries for therapeutic antibody discovery
Published in mAbs, 2023
GPCR represents a class of seven transmembrane receptors. GPCRs have been recognized as successful drug targets as approximately one third of the US Food and Drug Administration (FDA)-approved drugs target GPCRs.159,160 However, due to high hydrophobicity, conformational flexibility, and limited accessibility of epitopes on the extracellular portion, GPCRs are challenging targets for antibodies. To date, there are only two FDA-approved antibodies drugs targeting GPCRs: mogamulizumab and erenumab, which target CC chemokine receptor 4 and calcitonin gene-related peptide receptor, respectively.161 Phage display offers a valuable antibody discovery platform for targeting challenging targets, including ion channels, transporters, and GPCRs.162 For example, one synthetic antibody phage display library was designed by mining the sequences of all known GPCR ligand interactions and incorporating the identified binding motifs into CDRH3. As a result, this GPCR-focused library successfully led to discovery of a panel of antagonistic antibodies targeting glucagon-like peptide-1 receptor with high affinity.15
Current and emerging drug treatment strategies for polycystic ovary syndrome
Published in Expert Opinion on Pharmacotherapy, 2023
Nafiye Helvaci, Bulent Okan Yildiz
Glucagon-like peptide-1 receptor agonists (GLP-1RAs) are a class of antidiabetic agents with incretin mimetic activity, augmentation of insulin and inhibition of glucagon secretion in a glucose-dependent manner. GLP-1RAs also have additional effects such as slowing gastric emptying and increasing satiety, thereby reducing food intake and inducing weight loss [58,59]. Besides, there is evidence indicating that these agents improve peripheral insulin sensitivity through several direct or indirect molecular pathways [60]. Because of these effects, GLP-1RAs are emerging as a therapeutic alternative for the management of overweight and obese women with PCOS. Moreover, GLP-1RAs have been shown to exert CV protective effects, which may be of particular importance in women with PCOS considering increased prevalence of multiple CV risk factors in this population [61].
Misrouting of glucagon and stathmin-2 towards lysosomal system of α-cells in glucagon hypersecretion of diabetes
Published in Islets, 2022
Farzad Asadi, Savita Dhanvantari
Studies have shown that glucagon secretion can be controlled by targeting mediators of intracellular signaling and exocytosis within the α-cell. Agonists of the glucagon-like peptide 1 receptor (GLP-1R) inhibit glucagon secretion by directly acting on α-cells, or indirectly through releasing insulin, Zn2+, and GABA from β-cells, or by releasing somatostatin from δ-cells.4 GABAA receptor agonists also directly inhibit glucagon secretion through binding with GABAA receptor on α-cells, increasing Cl− influx, and hyperpolarization of the plasma membrane.5,6 Antagonists of the glucose-dependent insulinotropic peptide receptor (GIP-R) directly suppress the glucagonotropic effect of GIP on α-cells.7 Insulin directly suppresses glucagon secretion through binding its receptor on α-cells8,9 or indirectly by increasing secretion of somatostatin from δ-cells.10 Blockers of KATP channels inactivate ion channels, and reduce α-cell electrical activity, which result in suppression of glucagon secretion.11–13 As well, in addition to blocking the effects of glucagon on hepatic glucose mobilization, anti- glucagon receptor antibodies may also block the autocrine effect of glucagon on glucagon secretion from α-cells.14,15