Results 101 to 110 of about 17,943 (269)

Divergence in μ and δ opioid receptor pharmacology in neurons and antinociceptive efficacy in neuropathic pain: Insights from MP135 and CYM51010

British Journal of Pharmacology, EarlyView.
Background and purpose Opioids targeting the μ opioid receptor remain largely ineffective in neuropathic pain conditions, emphasizing the need for novel therapeutic strategies. MP135 was reported to reduce thermal nociception in naive animals by activating μ‐δ opioid receptor heteromers.
Perrine Inquimbert, Chantal Fitterer, Sylvain Hugel, Mila Jesic, Yannick Goumon, Virgine Andry, Severine Schneider, Francois Daubeuf, Abdelfattah Faouzi, Stephane Doridot, Susruta Majumdar, Frederic Bihel, Martine Schmitt, Dominique Massotte   +13 more
wiley   +1 more source

Phosphorylation-induced conformation of beta(2)-adrenoceptor related to arrestin recruitment revealed by NMR [PDF]

, 2018
The C-terminal region of G-protein-coupled receptors (GPCRs), stimulated by agonist binding, is phosphorylated by GPCR kinases, and the phosphorylated GPCRs bind to arrestin, leading to the cellular responses.
Imai, Shunsuke, Iwai, Hideo, Kofuku, Yutaka, Mizukoshi, Toshimi, Nakata, Kunio, Natsume, Mei, Shimada, Ichio, Shiraishi, Yutaro, Ueda, Takumi   +8 more
core   +2 more sources

Profiling of HCAR1 signalling reveals Gαi/o and Gαs activation without β‐arrestin recruitment and the discovery of an allosteric agonist

British Journal of Pharmacology, EarlyView.
Abstract Background and Purpose Lactate, historically viewed as a metabolic by‐product, has emerged as a signalling molecule via the G protein–coupled receptor Hydroxycarboxylic Acid Receptor 1 (HCAR1). The receptor is primarily expressed in adipocytes but also found in various other tissues.
Simon Lind, Shane C. Wright, Emilia Gvozdenovic, Kristina Nilsson, Kenneth L. Granberg, Michel Bouvier, Linda C. Johansson   +6 more
wiley   +1 more source

Comprehensive transduceromic profiling of NOP receptor ligands at different Gα subunits

British Journal of Pharmacology, EarlyView.
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

β Arrestin inhibition induces autophagy, apoptosis, G0/G1 cell cycle arrest in agonist activated V2R receptor in breast cancer cells [PDF]

, 2021
Mohamed Hessien, Thoria Donia, Mohamed Kelany, Mohamed Abouda   +3 more
openalex   +1 more source

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

British Journal of Pharmacology, EarlyView.
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

ArreSTick motif controls β-arrestin-binding stability and extends phosphorylation-dependent β-arrestin interactions to non-receptor proteins

Cell Reports
Summary: The binding and function of β-arrestins are regulated by specific phosphorylation motifs present in G protein-coupled receptors (GPCRs).
András Dávid Tóth, Eszter Soltész-Katona, Katalin Kis, Viktor Guti, Sharon Gilzer, Susanne Prokop, Roxána Boros, Ádám Misák, András Balla, Péter Várnai, Lilla Turiák, András Ács, László Drahos, Asuka Inoue, László Hunyady, Gábor Turu   +15 more
doaj   +1 more source

Pharmacological and genetic manipulations at the µ-opioid receptor reveal arrestin-3 engagement limits analgesic tolerance and does not exacerbate respiratory depression in mice [PDF]

, 2021
He Li, Sarah W. Gooding, Elinor Lewis, Lindsey Felth, Anirudh Gaur, Jennifer L. Whistler   +5 more
openalex   +1 more source

Lock, relax, load, and shoot: a molecular perspective on Nedd4 regulation

The FEBS Journal, EarlyView.
Structural basis of inactive and active states of the Nedd4 HECT E3 ligase subfamily, following a ‘lock, relax, load, and shoot’ mechanism. In the locked, autoinhibited state, intramolecular domain interactions restrain the HECT domain. Relaxation releases these restraints, allowing loading of ubiquitin onto the catalytic cysteine, followed by the ...
Masa Janosev, Tomas Obsil, Veronika Obsilova   +2 more
wiley   +1 more source

Comparative interactome analysis of α-arrestin families in human and Drosophila

eLife
The α-arrestins form a large family of evolutionally conserved modulators that control diverse signaling pathways, including both G-protein-coupled receptor (GPCR)-mediated and non-GPCR-mediated pathways, across eukaryotes.
Kyung-Tae Lee, Inez KA Pranoto, Soon-Young Kim, Hee-Joo Choi, Ngoc Bao To, Hansong Chae, Jeong-Yeon Lee, Jung-Eun Kim, Young V Kwon, Jin-Wu Nam   +9 more
doaj   +1 more source