Results 91 to 100 of about 12,251 (147)

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

Concepts of GPCR-controlled navigation in the immune system

, 2019
G-protein-coupled receptor (GPCR) signaling is essential for the spatiotemporal control of leukocyte dynamics during immune responses. For efficient navigation through mammalian tissues, most leukocyte types express more than one GPCR on their surface ...
Boneschansker L, Brandt SL, Chan EC, Filippo K, Freedman NJ, Hjorto GM, Hons M, Katakai T, Kitayama J, Lemos C, Ley K, Miyabe Y, Moussavi‐Harami SF, Proudfoot AEI, Purvanov V, Rot A, Scheiermann C, Schwarz J, Sokol CL, Sotsios Y, Steury MD, Takeda A, Thiriot A, Tomhave ED, Wang Y, Yanagihara S, Zhang Y   +26 more
core   +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

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

PAR1 Agonists Stimulate APC-Like Endothelial Cytoprotection and Confer Resistance to Thromboinflammatory Injury [PDF]

, 2018
Stimulation of protease-activated receptor 1 (PAR1) on endothelium by activated protein C (APC) is protective in several animal models of disease, and APC has been used clinically in severe sepsis and wound healing.
Aisiku, Omozuanvbo, Ceunynck, Karen De, Chaudhry, Sharjeel A., Dockendorff, Chris, Fitch-Tewfik, Jennifer L., Flaumenhaft, Robert, Higgins, Sarah J., Ingber, Donald E., Jain, Abhishek, Parikh, Samir M., Peters, Christian G.   +10 more
core   +1 more source

PDE4D and PDE3B orchestrate distinct cAMP microdomains in 3T3‐L1 adipocytes

British Journal of Pharmacology, EarlyView.
Basal conditions: •Ins/PDE3B lowers cytoplasmic cAMP (cyt‐cAMP) without affecting plasma membrane cAMP (pm‐cAMP). •Insulin decreases lipid droplet cAMP (LD‐cAMP) independent of PDE3B. •FGF1/PDE4D modestly reduces both cyt‐ and pm‐cAMP, while PDE4D alone can modulate LD‐cAMP. ISO stimulation: •Ins/PDE3B has minimal impact on cyt‐cAMP.
Johannes Krier, David Spähn, David Arturo Juarez Lopez, Judith L. Nono, Judith Seigner, Lisa Jacob, Siegfried Ussar, Robert Lukowski, Andreas L. Birkenfeld, Gencer Sancar   +9 more
wiley   +1 more source

Usefulness for the combination of G protein- and β-arrestin-biased ligands of μ-opioid receptors: Prevention of antinociceptive tolerance

Molecular Pain, 2017
Background µ-Opioid receptor internalization is considered to be critically linked to antinociceptive tolerance. Although µ-opioid receptor agonists have been administered simultaneously with other drugs to control pain, little information is available ...
Tomohisa Mori, Naoko Kuzumaki, Takamichi Arima, Michiko Narita, Ryunosuke Tateishi, Takashige Kondo, Yusuke Hamada, Hirotsugu Kuwata, Miho Kawata, Mitsuaki Yamazaki, Kazuyuki Sugita, Akinobu Matsuzawa, Kanae Baba, Takayasu Yamauchi, Kimio Higashiyama, Miki Nonaka, Kanako Miyano, Yasuhito Uezono, Minoru Narita   +18 more
doaj   +1 more source

Cannabigerol reverses mechanical allodynia through α2A‐adrenergic modulation of thalamocortical signaling in chemotherapy‐induced neuropathy

British Journal of Pharmacology, EarlyView.
Abstract Background and Purpose Chemotherapy‐induced peripheral neuropathy (CIPN) is a prevalent and treatment‐resistant side effect of platinum‐based chemotherapy, characterised by mechanical allodynia. Cannabigerol (CBG), a non‐psychoactive cannabinoid, has shown antinociceptive potential, but its site and mechanism of action remain unclear.
Quinn W. Wade, Nathan Morris, Diana E. Sepulveda, Alonso Cortez‐Resendiz, Christopher Brandl, Jennifer E. Lausch, Mariya Starostina, Nicholas M. Graziane   +7 more
wiley   +1 more source

A new inhibitor of the β-arrestin/AP2 endocytic complex reveals interplay between GPCR internalization and signalling

Nature Communications, 2017
Beta-arrestins play central roles in the mechanisms regulating GPCR signalling and trafficking. Here the authors identify a selective inhibitor of the interaction between β-arrestin and the β2-adaptin subunit of the clathrin adaptor protein AP-2, which ...
Alexandre Beautrait, Justine S. Paradis, Brandon Zimmerman, Jenna Giubilaro, Ljiljana Nikolajev, Sylvain Armando, Hiroyuki Kobayashi, Lama Yamani, Yoon Namkung, Franziska M. Heydenreich, Etienne Khoury, Martin Audet, Philippe P. Roux, Dmitry B. Veprintsev, Stéphane A. Laporte, Michel Bouvier   +15 more
doaj   +1 more source

Pepducin-mediated cardioprotection via β-arrestin-biased β2-adrenergic receptor-specific signaling [PDF]

, 2018
Reperfusion as a therapeutic intervention for acute myocardial infarction-induced cardiac injury itself induces further cardiomyocyte death. β-arrestin (βarr)-biased β-adrenergic receptor (βAR) activation promotes survival signaling responses in vitro ...
Benovic, Jeffrey L., Carter, Rhonda L., de Lucia, Claudio, Gao, Erhe, Grisanti, Laurel A., Koch, Walter J., Thomas, Toby P., Tilley, Douglas G.   +7 more
core   +1 more source