Results 41 to 50 of about 18,493 (159)
Functional selectivity of EM-2 analogs at the mu-opioid receptor
Frontiers in Pharmacology, 2023 The mu opioid receptor agonists are the most efficacious pain controlling agents but their use is accompanied by severe side effects. More recent developments indicate that some ligands can differentially activate receptor downstream pathways, possibly ...
Justyna Piekielna-Ciesielska +6 more
doaj +1 more source
International Journal of Cancer, EarlyView.ABSTRACT Somatostatin receptors (SSTR) mediate the antiproliferative, antisecretory, and proapoptotic effects of somatostatin and its synthetic analogs. Their surface expression on neuroendocrine tumor (NET) cells is required for somatostatin analog therapy and radiopharmaceutical therapy (RPT).
Neeraj Kumari +10 more
wiley +1 more source
Molecules, 2021 The δ-opioid receptor (δOR) holds great potential as a therapeutic target. Yet, clinical drug development, which has focused on δOR agonists that mimic the potent and selective tool compound SNC80 have largely failed.
Yazan J. Meqbil +7 more
doaj +1 more source
The Endothelial CXCR Family in Vascular Health and Disease
iNew Medicine, EarlyView.ABSTRACT Endothelial cells (ECs) form the dynamic interface between blood and tissue, serving as key regulators of vascular homeostasis, inflammation, and repair. Among the molecular systems governing endothelial behavior, the C‐X‐C motif chemokine receptor (CXCR) family—originally characterized in immunology for its roles in leukocyte trafficking and ...
Zhiming Wu +4 more
wiley +1 more source
Brazilian Journal of Medical and Biological Research, 2013 β-arrestins are expressed proteins that were first described, and are well-known, as negative regulators of G protein-coupled receptor signaling.
J. Zhan +5 more
doaj +1 more source
Sodium Ions Affect GPR17 Conformational States and Functionality
Proteins: Structure, Function, and Bioinformatics, EarlyView.ABSTRACT Sodium is an allosteric modulator of several class‐A GPCR regulating active versus inactive conformation state and may be a critical issue for the optimization of crystallization procedures. Herein, the role of Na+ in the regulation of GPR17 conformational states was studied through MD simulations of GPR17 wild‐type and mutated on two ...
Luca Palazzolo +6 more
wiley +1 more source
Inhibitory Effect of CCK-8 on Methamphetamine-Induced Apoptosis
Fayixue Zazhi, 2021 ObjectiveTo investigate the inhibitory effect of cholecystokinin octapeptide （CCK-8） binding to cholecystokinin 2 receptor （CCK2R） on methamphetamine （METH）-induced neuronal apoptosis, and to explore the signal transduction mechanism of β-arrestin 2 in ...
ZHANG Wu-hua +8 more
doaj +1 more source
Compartmentalisation in cAMP signalling: A phase separation perspective
British Journal of Pharmacology, EarlyView.Cells rely on precise spatiotemporal control of signalling pathways to ensure functional specificity. The compartmentalisation of cyclic AMP (cAMP) and protein kinase A (PKA) signalling enables distinct cellular responses within a crowded cytoplasmic space.
Milda Folkmanaite, Manuela Zaccolo
wiley +1 more source
β-arrestin 2 quenches TLR signaling to facilitate the immune evasion of EPEC
Gut Microbes, 2020 The protein translocated intimin receptor (Tir) from enteropathogenic Escherichia coli shares sequence similarity with the host cellular immunoreceptor tyrosine-based inhibition motifs (ITIMs).
Zijuan Chen +11 more
doaj +1 more source
The potential for biased signalling in the P2Y receptor family of GPCRs
British Journal of Pharmacology, EarlyView.The purinergic receptor family is primarily activated by nucleotides, and contains members of both the G protein coupled‐receptor (GPCR) superfamily (P1 and P2Y) and ligand‐gated ion channels (P2X). The P2Y receptors are widely expressed in the human body, and given the ubiquitous nature of nucleotides, purinergic signalling is involved with a plethora
Claudia M. Sisk +2 more
wiley +1 more source