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Design, Structure-Activity Relationships, and Computational Modeling Studies of a Series of α-Helix Biased, Ultra-Short Glucagon-like Peptide-1 Receptor Agonists.
Molecules
December 2024
Resolute Bio, 48 Dunham Rd., Suite 5400, Beverly, MA 01915, USA.
A systematic structure-activity and computational modeling analysis of a series of glucagon-like peptide-1 receptor (GLP-1R) agonists based upon an ultra-short GLP-1 peptide, H-His-Aib-Glu-Gly-Thr-Phe-Thr-Ser-Asp-Bip-Bip-NH2, was conducted. This highly potent 11-mer peptide led to a deeper understanding of the α-helical bias of strategic α-methylation within the linear parent template as well as optimization of GLP-1R agonist potency by 1000-fold. These data were correlated with previously reported co-structures of both full-length GLP-1 analogs and progenitor N-terminal GLP-1 fragment analogs related to such ultra-short GLP-1R agonist peptides.
View Article and Find Full Text PDFGlucagon-like peptide-1 receptor agonists and upper endoscopy: a real-world experience.
Obesity (Silver Spring)
January 2025
Division of Gastroenterology, Hepatology and Endoscopy, Brigham and Women's Hospital, Boston, Massachusetts, USA.
Objective: Increased use of glucagon-like peptide-1 receptor agonists (GLP-1RAs) has raised safety concerns during endoscopy due to their mechanism of delaying gastric emptying. This study aims to evaluate the impact of GLP-1RAs on technical success and safety of esophagogastroduodenoscopy (EGD).
Methods: This was a retrospective study of bariatric patients who underwent EGD between January 2022 and December 2023.
High-Throughput Screening of DPPIV Inhibitors Antagonizing GLP-1 Degradation Using an Enzymatic Activated Fluorescent Probe.
Anal Chem
January 2025
First Affiliated Hospital, College of Integrative Medicine, College of Pharmacy, Dalian Medical University, Dalian 116044, China.
Dipeptidyl peptidase IV (DPPIV, EC 3.4.14.
View Article and Find Full Text PDFDipeptidyl peptidase-4 inhibitor linagliptin reduces inflammatory response, ameliorates tissue edema formation, and improves survival in severe sepsis.
Biomed Pharmacother
January 2025
Department of Research, Mount Sinai Medical Center, Miami Beach, FL, USA. Electronic address:
Background: Excessive inflammation in sepsis causes microvascular dysfunction associated with organ dysfunction and high mortality. The present studies aimed to examine the therapeutic potential of linagliptin, a dipeptidyl peptidase-4 (DPP-4) inhibitor in a clinically relevant polymicrobial sepsis model in mice.
Methods: Sepsis was induced by cecal ligation and puncture (CLP).
The Use of Single Pass Albumin Dialysis and Hemoadsorption in Management of Life-Threatening Amlodipine Overdose.
Semin Dial
December 2024
Department of Paediatrics and Adolescent Medicine, Hong Kong Children's Hospital, Hong Kong.
We report the successful application of single pass albumin dialysis (SPAD) and hemoadsorption (HA) in two teenagers with amlodipine poisoning. A 16-year-old girl with amlodipine overdose developed refractory shock and lactic acidosis despite multiple inotropes, calcium, insulin, and glucagon infusion. SPAD was initiated 18 h after the incident for 21 h.
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