A5081715819- Diabetes Treatment and Management
- Cancer, Lipids, and Metabolism
- Receptor Mechanisms and Signaling
- Pancreatic function and diabetes
- Histone Deacetylase Inhibitors Research
- Inflammatory mediators and NSAID effects
- Neuropeptides and Animal Physiology
- Adenosine and Purinergic Signaling
- Metal complexes synthesis and properties
- Antibiotic Use and Resistance
- Synthesis and Biological Activity
- Antibiotic Resistance in Bacteria
- Lipoproteins and Cardiovascular Health
- Cancer, Hypoxia, and Metabolism
- Urinary Tract Infections Management
- GDF15 and Related Biomarkers
- Cellular transport and secretion
Institute of Life Sciences
2017-2024
Manipal Academy of Higher Education
2020-2024
University of Hyderabad
2017-2024
Vanderbilt University Medical Center
2023
Upon activation, G protein coupled receptors (GPCRs) associate with heterotrimeric proteins at the plasma membrane to initiate second messenger signaling. Subsequently, activated receptor experiences desensitization, internalization, and recycling back membrane, or it undergoes lysosomal degradation. Recent reports highlight specific cases of persistent cyclic AMP generation by internalized GPCRs, although functional significance mechanistic details remain be defined. Cyclic from...
Given its glycemic efficacy and ability to reduce the body weight, glucagon-like peptide 1 receptor (GLP-1R) agonism has emerged as a preferred treatment for diabetes associated with obesity. We here report that small-molecule Class histone deacetylase (HDAC) inhibitor Entinostat (MS-275) enhances GLP-1R potentiate glucose-stimulated insulin secretion decrease weight in diet-induced obese (DIO) mice. MS-275 is not an agonist or allosteric activator of but sustained receptor-mediated...
Replacement of the tryptophan cage (Trp-cage) with C-terminal oxyntomodulin undecapeptide along tyrosine substitution at amino terminus converts selective glucagon-like peptide-1 receptor (GLP-1R) agonist exendin-4 to a novel GLP-1R and GIPR dual I-M-150847. Reduced internalization incretin receptors upon activation by I-M-150847 promotes iterative signaling that enhances effect reverses obesity.
Abstract We report the discovery of a novel unimolecular glucagon-like peptide-1 (GLP-1) and glucose-dependent insulinotropic polypeptide (GIP) receptor dual agonist that exhibits potent glycemic control weight loss in diet-induced obese mice. The agonism GLP-1 GIP was achieved by replacing tryptophan cage exendin-4 with C-terminal undecapeptide sequence oxyntomodulin along single amino acid substitution from histidine to tyrosine at terminus peptide. structural modification places lysine 30...