Results 81 to 90 of about 31,759 (252)

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, Simona Daniele, Davide Bianchi, Lara Russo, Stefano Capaldi, Maria Letizia Trincavelli, Ivano Eberini   +6 more
wiley   +1 more source

A small molecule enhances arrestin-3 binding to the β2-adrenergic receptor

Communications Chemistry
Excessive signaling by various GPCRs underlies a variety of human disorders. Suppression of GPCRs by “enhanced” arrestin mutants was proposed as therapy.
Han Kurt, Ali Akyol, Cagdas Devrim Son, Chen Zheng, Irene Gado, Massimiliano Meli, Erica Elisa Ferrandi, Ivan Bassanini, Francesca Vasile, Vsevolod V. Gurevich, Aylin Nebol, Esra Cagavi, Giulia Morra, Ozge Sensoy   +13 more
doaj   +1 more source

G-Protein/β-Arrestin-Linked Fluctuating Network of G-Protein-Coupled Receptors for Predicting Drug Efficacy and Bias Using Short-Term Molecular Dynamics Simulation.

, 2016
The efficacy and bias of signal transduction induced by a drug at a target protein are closely associated with the benefits and side effects of the drug.
Osamu Ichikawa (3169788), Atsushi Yamada, Kazuto Yamazaki (9494), Atsushi Yamada (282892), Kazushi Fujimoto, Kazushi Fujimoto (1730860), Susumu Okazaki, Kazuto Yamazaki, Susumu Okazaki (3169791), Osamu Ichikawa   +9 more
core   +1 more source

Spatiotemporal Expression of ARRDC5 in Mammalian Spermatogenesis

Andrology, EarlyView.
ABSTRACT Background Spermiogenesis is the final phase of sperm development during which haploid round spermatids transform into specialized spermatozoa and occurs across distinct stages of sperm production in the seminiferous epithelium. Abnormalities in this process lead to malformations and an inability of sperm to fertilize eggs.
LeeLa D. Robinson, Jon M. Oatley
wiley   +1 more source

Melanopsin co-localizes with β-arrestin 1 and β-arrestin 2 in ipRGCs.

, 2014
(A–C) Three major nuclear layers of the mouse retina defined by DAPI (GCL, Ganglion cell layer; INL, Inner nuclear layer; PRL, Photoreceptor layer). (A) Visual arrestin staining localized in the PRL outer segments.
Phyllis R. Robinson (204369), Evan G. Cameron (662130)   +1 more
core   +1 more source

β-Arrestins in the Immune System [PDF]

, 2013
β-Arrestins regulate G protein-coupled receptors through receptor desensitization while also acting as signaling scaffolds to facilitate numerous effector pathways. Recent studies have provided evidence that β-arrestins play a key role in inflammatory responses.
Dianhua, Jiang, Ting, Xie, Jiurong, Liang, Paul W, Noble   +3 more
openaire   +2 more sources

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

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, Simon Pitchford, Graham Ladds   +2 more
wiley   +1 more source

Engineered hyperphosphorylation of the 2-adrenoceptor prolongs arrestin-3 binding and induces arrestin internalization

, 2015
G protein-coupled receptor phosphorylation plays a major role in receptor desensitization and arrestin binding. It is, however, unclear how distinct receptor phosphorylation patterns may influence arrestin binding and subsequent trafficking.
Al-Sabah, Suleiman, Butcher, Adrian J., Zindel, Diana, Krasel, Cornelius, Bunemann, Moritz, Tobin, Andrew B., Lanzerstorfer, Peter, Weghuber, Julian   +7 more
core   +1 more source

Homodimerization of CB2 cannabinoid receptor triggered by a bivalent ligand enhances cellular signaling

Pharmacological Research
G protein-coupled receptors (GPCRs) exist within a landscape of interconvertible conformational states and in dynamic equilibrium between monomers and higher-order oligomers, both influenced by ligand binding.
Gemma Navarro, Marc Gómez-Autet, Paula Morales, Joan Biel Rebassa, Claudia Llinas del Torrent, Nadine Jagerovic, Leonardo Pardo, Rafael Franco   +7 more
doaj   +1 more source