Results 111 to 120 of about 12,251 (147)

Mechanistic insights into the versatile stoichiometry and biased signaling of the apelin receptor-arrestin complex

Nature Communications
The apelin receptor (APJR) plays a pivotal role in regulating cardiovascular and metabolic health1,2. Understanding the mechanisms of biased agonism at APJR is crucial for drug discovery, as stimulation of the β-arrestin pathway may lead to some adverse ...
Yang Yue, Chanjuan Xu, Lijie Wu, Man Na, Kexin Xu, Xuan Chen, Yuxuan Song, Sichun Weng, Lu Xu, Fei Li, Xi Lin, Arthur Wang, Jianfeng Liu, Fei Xu   +13 more
doaj   +1 more source

Evidence for a Two‐Step Model for Activation of GPR25 by the Chemoattractant CXCL17

Basic &Clinical Pharmacology &Toxicology, Volume 139, Issue 1, July 2026.
ABSTRACT CXCL17 was recently reported to activate GPR25, a receptor expressed by T‐regulatory cells. Although classified as a chemokine, the activity of CXCL17 is ablated by minor C‐terminal truncation, suggesting a novel mode of receptor activation. We set out to test this hypothesis by mutagenesis. GPR25 was expressed in the murine pre‐B cell line L1.
Wuqing Yang, Sean P. Giblin, James E. Pease   +2 more
wiley   +1 more source

Harnessing Fatty Acid By‐Products for Diabetes Management: Insights From Nutritional and Biological Research

eFood, Volume 7, Issue 3, June 2026.
Bioactive fatty acids from agro‐industrial byproducts are highlighted as a promising avenue for managing diabetes in this review, which aims to develop targeted interventions for optimal utilization and therapeutic benefits. ABSTRACT Diabetes mellitus (DM), influenced by multifaceted factors, creates a complex imbalance within the body. Nutrition plays
Youssef Elouafy, Abdelaali Balahbib, Meriem El Fessikh, Saïd Gharby, Nasreddine El Omari, Waleed Al Abdulmonem, Gokhan Zengin, Abdelhakim Bouyahya   +7 more
wiley   +1 more source

Clinical dilemma of mood stabilizer augmentation in treatment‐resistant schizophrenia with residual phase: A case report of valproate‐associated hypoglycemia and cytopenia, and subsequent lithium response

Psychiatry and Clinical Neurosciences Reports, Volume 5, Issue 2, June 2026.
Abstract Background Mood stabilizer augmentation is frequently used in treatment‐resistant schizophrenia despite limited guideline recommendations. Evidence for its efficacy and safety in the residual phase, however, remains insufficient. Case Presentation A 49‐year‐old Japanese woman with treatment‐resistant residual schizophrenia exhibited persistent
Yoshiki Kasagi, Naomichi Okamoto, Reiji Yoshimura   +2 more
wiley   +1 more source

ATHENA: A Phase 3, Open-Label Study Of The Safety And Effectiveness Of Oliceridine (TRV130), A G-Protein Selective Agonist At The µ-Opioid Receptor, In Patients With Moderate To Severe Acute Pain Requiring Parenteral Opioid Therapy. [PDF]

, 2019
Background:Pain management with conventional opioids can be challenging due to dose-limiting adverse events (AEs), some of which may be related to the simultaneous activation of β-arrestin (a signaling pathway associated with opioid-related AEs) and G ...
Beard, Timothy L, Bergese, Sergio D, Berkowitz, Richard D, Brzezinski, Marek, Cochrane, Kristina, Habib, Ashraf S, Hammer, Gregory B, Mace, Sharon E, Minkowitz, Harold S, Pan, Peter H, Wase, Linda   +10 more
core  

Omega‐3 DHA as a blank canvas: A molecular approximation to how lipid mediators modulate LGR6 in inflammation resolution

Protein Science, Volume 35, Issue 6, June 2026.
Abstract The leucine‐rich repeat‐containing G protein‐coupled receptor 6 (LGR6) has a potential role in inflammation resolution and different cancer processes. In this study, we employed computational techniques, including molecular docking and molecular dynamics simulations of mammalian membrane‐embeded systems, to understand the activation mechanism ...
Álex Pérez‐Sánchez, Mireia Garcia‐Viloca, Àngels González‐Lafont, José M. Lluch   +3 more
wiley   +1 more source

Intrinsic conformational equilibria position arrestin‐2 for activation

Protein Science, Volume 35, Issue 6, June 2026.
Abstract Arrestins regulate G protein‐coupled receptor (GPCR) signaling by undergoing large‐scale conformational rearrangements, yet the solution‐state equilibria that underlie arrestin pre‐activation remain poorly defined. While prior studies identified slow conformational exchange at the interdomain interface, these minor states could not be ...
Tucker J. Shriver, Kerem Kahraman, Mingzhe Pan, Çağdaş Dağ, Marco Tonelli, Scott A. Robson, Joshua J. Ziarek   +6 more
wiley   +1 more source

Fluorescence correlation spectroscopy, combined with bimolecular fluorescence complementation, reveals the effects of β-arrestin complexes and endocytic targeting on the membrane mobility of neuropeptide Y receptors [PDF]

, 2012
Fluorescence correlation spectroscopy (FCS) and photon counting histogram (PCH) analysis are powerful ways to study mobility and stoichiometry of G protein coupled receptor complexes, within microdomains of single living cells.
Briddon, Stephen J., Holliday, Nicholas D., Kilpatrick, Laura E.   +2 more
core  

Comprehensive transduceromic profiling of NOP receptor ligands at different Gα subunits

British Journal of Pharmacology, Volume 183, Issue 12, Page 3195-3212, June 2026.
Abstract Background and Purpose The nociceptin/orphanin FQ (N/OFQ) peptide receptor (NOP) is an opioid receptor family member with distinct pharmacology and broad therapeutic potential. NOP receptors regulate functions such as nociception, stress reactivity, reward, mood, autonomic tone, immunity and sleep/wake cycle.
Davide Malfacini, Riccardo Camilotto, Michele Maritan, Erika Morrone, Stephen Afriyie Boateng, Anna Vacilotto, Salvatore Pacifico, Remo Guerrini, Nurulain T. Zaveri, Girolamo Calo'   +9 more
wiley   +1 more source

GRKs and arrestins: Nomenclature and functions in GPCR‐dependent and ‐independent signalling

British Journal of Pharmacology, Volume 183, Issue 11, Page 2619-2633, June 2026.
G protein‐coupled receptor (GPCR) kinases (GRKs) and arrestins play a critical role in the regulation of GPCR signalling. Historic names of mammalian GRKs were replaced by systematic ones in the 1990s; however, both kinds of names are currently in use for mammalian arrestins.
Vsevolod V. Gurevich
wiley   +1 more source