Results 161 to 170 of about 11,641 (225)

Second‐generation prokineticin PKR1 receptor agonists: Advancing cardioprotection against chemotherapy‐induced toxicity

British Journal of Pharmacology, Volume 183, Issue 12, Page 3377-3394, June 2026.
IS39, a novel non‐peptide PKR1 agonist, confers cardioprotection against doxorubicin‐induced toxicity. IS39 activates PKR1‐mediated pro‐survival signalling in cardiomyocytes, reducing reactive oxygen species (ROS), DNA damage and fibrosis markers. In vivo, IS39 preserves cardiac geometry and function in mice exposed to chronic doxorubicin challenge ...
Anais Audebrand, Simone Brogi, Mustafa Tezeren, Andrea Tafi, Omer H. Ocak, Hasan Koyuncu, Igor Tetko, Laurent Désaubry, Canan G. Nebigil   +8 more
wiley   +1 more source

Unimolecular GLP‐1/Apelin Hybrid Peptides Cause Prominent Appetite Suppression, as Well as Enhancing Insulin Secretion, Beta‐Cell Survival and Glycaemic Regulation

Diabetes, Obesity and Metabolism, Volume 28, Issue 6, Page 4706-4717, June 2026.
ABSTRACT Aim To characterise the metabolic benefits of a GLP‐1/apelin hybrid peptide, namely exendin‐4‐linker‐apelin (ELA), and associated acylated forms, including ELA‐Lys12(γGluPal), ELA‐Lys27(γGluPal) and ELA‐Lys38(γGluPal). Methods Concentration‐ and receptor‐dependent effects of the peptides on insulin secretion and beta‐cell turnover were ...
Ananyaa Sridhar, Ethan S. Palmer, Sarah L. Craig, Elzbieta Krason‐Kidzinska, Nigel Irwin, Finbarr P. M. O'Harte   +5 more
wiley   +1 more source

Cellular Electrical Impedance as a Method to Decipher CCR7 Signalling and Biased Agonism. [PDF]

Int J Mol Sci, 2022
Vanalken N, Boon K, Doijen J, Schols D, Van Loy T.   +4 more
europepmc   +1 more source

Photocaged Oxytocin and Vasopressin Probes to Decipher Neuropeptide Signalling With High Spatiotemporal Resolution

Angewandte Chemie International Edition, Volume 65, Issue 22, 25 May 2026.
Novel and biocompatible photoactivatable oxytocin and vasopressin probes, utilising state‐of‐the‐art photocages, remain inactive in the dark. Light exposure facilitates rapid spatiotemporal receptor activation and phospholipase C (PLC)‐mediated downstream signalling. Figure created in https://BioRender.com.
Konstantin Raabe, Predrag Kalaba, Xuan Ling Hilary Yong, Greta Crudeli, Sarah Melzer, Erik Keimpema, Victor Anggono, Markus Muttenthaler   +7 more
wiley   +1 more source

Monoclonal Antibody 5F1 Modulates Formyl Peptide Receptor 1 Conformation for Transmembrane Signaling

FASEB BioAdvances
Formyl peptide receptor 1 (FPR1) is a G protein‐coupled receptor (GPCR) that mediates chemotaxis and bactericidal activities in phagocytes. The monoclonal antibody 5F1 is generated against full‐length FPR1 and used widely for detection of FPR1 expression.
Yue Wang, Yezhou Liu, Yixin Chang, Richard D. Ye   +3 more
doaj   +1 more source

Quantitative Systems Pharmacology and Biased Agonism at Opioid Receptors: A Potential Avenue for Improved Analgesics. [PDF]

Int J Mol Sci, 2022
Bedini A, Cuna E, Baiula M, Spampinato S.   +3 more
europepmc   +1 more source

Structural Insights into Ligand-Receptor Interactions Involved in Biased Agonism of G-Protein Coupled Receptors. [PDF]

Molecules, 2021
Jóźwiak K, Płazińska A.
europepmc   +1 more source

Editorial: Recent Advances in G Protein-Coupled Receptor Signalling: Impact of Intracellular Location, Environment and Biased Agonism. [PDF]

Front Pharmacol, 2021
Halls ML, Davenport AP, Summers RJ.
europepmc   +1 more source

Actions of Novel Angiotensin Receptor Blocking Drugs, Bisartans, Relevant for COVID-19 Therapy: Biased Agonism at Angiotensin Receptors and the Beneficial Effects of Neprilysin in the Renin Angiotensin System. [PDF]

Molecules, 2022
Moore GJ, Ridgway H, Kelaidonis K, Chasapis CT, Ligielli I, Mavromoustakos T, Bojarska J, Matsoukas JM.   +7 more
europepmc   +1 more source

Novel glucagon-like peptide-1 analogue exhibits potency-driven G-protein biased agonism with promising effects on diabetes and diabetic dry eye syndrome. [PDF]

Bioengineered, 2022
Hao Y, Wei M, Zhang N, Zhang X.
europepmc   +1 more source