Results 81 to 90 of about 17,943 (269)

β-arrestin1 and 2 exhibit distinct phosphorylation-dependent conformations when coupling to the same GPCR in living cells

Nature Communications, 2022
Here the authors present improved intramolecular sensors for β-arrestin2 and 1, which enable assessment of conformational changes of both isoforms in living cells.
Raphael S. Haider, Edda S. F. Matthees, Julia Drube, Mona Reichel, Ulrike Zabel, Asuka Inoue, Andy Chevigné, Cornelius Krasel, Xavier Deupi, Carsten Hoffmann   +9 more
doaj   +1 more source

Identification of chemokine receptors as potential modulators of endocrine resistance in oestrogen receptor–positive breast cancers [PDF]

, 2014
Introduction Endocrine therapies target oestrogenic stimulation of breast cancer (BC) growth, but resistance remains problematic. Our aims in this study were (1) to identify genes most strongly associated with resistance to endocrine therapy by ...
A Boudot, A Levoye, AE Gururaj, AH Evans, AK Dunbier, Anita Dunbier, Aradhana Rani, AS Coutts, B Györffy, BC Nair, CA Moore, CM Chan, DG Duda, EA Musgrove, F Andre, GJ Sabnis, H Shankar, H Zheng, J Kang, J Xu, JM Burns, K Hattermann, K Sauvé, KE Luker, LA Martin, LA Martin, LA Martin, Lesley-Ann Martin, LV Rhodes, M Dowsett, Mitch Dowsett, MJ Ellis, MR Hara, MT Weigel, N Lapteva, OE Hawkins, Qiong Gao, R Santen, RD Berahovich, Ricardo Ribas, RK Singh, S Ali, S Masamura, S Masri, S Rajagopal, SE Ghayad, SM DeWire, Sunil Pancholi, TJ Frederick, TN Hartmann, V Lakshmikanthan, Y Shi, YC Su, Z Liang, Zara Ghazoui   +54 more
core   +1 more source

Neuropsychopharmacology of hallucinogenic and non‐hallucinogenic 5‐HT2A receptor agonists

British Journal of Pharmacology, EarlyView.
Psychedelic drugs such as LSD and psilocin were once relegated to the fringes of medical research because of their association with counterculture movements and a perceived concern about harm through recreational use, and their consequent legal prohibition in the early 1970s.
Trevor Sharp, Aurelija Ippolito
wiley   +1 more source

Uncovering missing pieces: duplication and deletion history of arrestins in deuterostomes

BMC Evolutionary Biology, 2017
Background The cytosolic arrestin proteins mediate desensitization of activated G protein-coupled receptors (GPCRs) via competition with G proteins for the active phosphorylated receptors.
Henrike Indrischek, Sonja J. Prohaska, Vsevolod V. Gurevich, Eugenia V. Gurevich, Peter F. Stadler   +4 more
doaj   +1 more source

Evidence that 5‐HT2A receptor signalling efficacy and not biased agonism differentiates serotonergic psychedelic from non‐psychedelic drugs

British Journal of Pharmacology, EarlyView.
Background and Purpose Serotonergic psychedelic drugs are under investigation as therapies for various psychiatric disorders, including major depression. Although serotonergic psychedelic drugs are 5‐HT2A receptor agonists, some such agonists are not psychedelic, potentially due to differences in 5‐HT2A receptor ligand bias or signalling efficacy. Here,
Aurelija Ippolito, Sridhar Vasudevan, Shaun Hurley, Gary Gilmour, Frederick Westhorpe, Grant Churchill, Trevor Sharp   +6 more
wiley   +1 more source

Cannabinoid CB1 and CB2 Receptor-Mediated Arrestin Translocation: Species, Subtype, and Agonist-Dependence

Frontiers in Pharmacology, 2019
Arrestin translocation and signaling have come to the fore of the G protein-coupled receptor molecular pharmacology field. Some receptor–arrestin interactions are relatively well understood and considered responsible for specific therapeutic or adverse ...
Mikkel Søes Ibsen, Mikkel Søes Ibsen, David B. Finlay, Monica Patel, Monica Patel, Jonathan A. Javitch, Jonathan A. Javitch, Michelle Glass, Natasha Lillia Grimsey, Natasha Lillia Grimsey   +9 more
doaj   +1 more source

Function and dynamics of the intrinsically disordered carboxyl terminus of β2 adrenergic receptor

Nature Communications, 2023
Advances in structural biology have provided important mechanistic insights into signaling by the transmembrane core of G-protein coupled receptors (GPCRs); however, much less is known about intrinsically disordered regions such as the carboxyl terminus (
Jie Heng, Yunfei Hu, Guillermo Pérez-Hernández, Asuka Inoue, Jiawei Zhao, Xiuyan Ma, Xiaoou Sun, Kouki Kawakami, Tatsuya Ikuta, Jienv Ding, Yujie Yang, Lujia Zhang, Sijia Peng, Xiaogang Niu, Hongwei Li, Ramon Guixà-González, Changwen Jin, Peter W. Hildebrand, Chunlai Chen, Brian K. Kobilka   +19 more
doaj   +1 more source

Emerging Roles of β-Arrestins [PDF]

Cell Cycle, 2006
Arrestins were originally characterized as structural adaptor proteins which modulate the desensitization and trafficking of seven-membrane-spanning receptors. From these seminal observations a multitude of novel functions for this gene family have arisen. Here we review the recently identified roles for beta-arrestin including its nuclear function and
F Gregory, Buchanan, Raymond N, DuBois
openaire   +2 more sources

Palmitoylation of human proteinase-activated receptor-2 differentially regulates receptor-triggered ERK1/2 activation, calcium signalling and endocytosis [PDF]

, 2011
hPAR2 (human proteinase-activated receptor-2) is a member of the novel family of proteolytically activated GPCRs (G-protein-coupled receptors) termed PARs (proteinase-activated receptors).
Alyn H. Morice, Andrew Botham, Bijlmakers, Blanpain, Bockaert, Bockaert, Bohm, Carvou, Compton, Compton, Compton, DeFea, Dery, Doi, Eason, Escriba, Hansen, Hawtin, Hayashi, Heuser, Jiang, Kawate, Klinger, Krasel, Krupnick, Kumar, Lafleur, Laura R. Sadofsky, Ma, McCoy, Melkonian, Moffett, Moffett, Molino, Moore, Munshi, Oh, Okamoto, Okamoto, Palmer, Percherancier, Petaja-Repo, Piersen, Ponimaskin, Qanbar, Rimoldi, Sadeghi, Seatter, Shenoy, Stalheim, Steven J. Compton, Wei, Xiaodan Guo, Yu Pei Xiao, Zoudilova   +54 more
core   +5 more sources

Are we hallucinating or can psychedelic drugs modulate the immune system to control inflammation?

British Journal of Pharmacology, EarlyView.
Psychedelic drugs that activate 5‐HT2A receptors have been long used for cultural, medicinal and recreational purposes. Interest in psychedelics for treating psychiatric disorders has resurged recently and is well documented; less well recognised are their anti‐inflammatory properties. Growing evidence now demonstrates that psychedelics modulate immune
Omar Qureshi, Jamie Cowley, Ashley Pegg, Alison J. Cooper, John Gordon, Catherine A. Brady, Antonio Belli, Sam Butterworth, Rachel Upthegrove, Nick Andrews, Nicholas M. Barnes   +10 more
wiley   +1 more source