Results 91 to 100 of about 29,885 (192)

Considering the role of Murine double minute 2 in the cardiovascular system [PDF]

, 2019
The E3 ubiquitin ligase Murine double minute 2 (MDM2) is the main negative regulator of the tumor protein p53 (TP53). Extensive studies over more than two decades have confirmed MDM2 oncogenic role through mechanisms both TP53-dependent and TP53 ...
Lam, Brian, Roudier, Emile
core   +1 more source

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

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

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

Modelling G protein-biased agonism using GLP-1 receptor C-terminal mutations

Molecular Metabolism
Background and aim: The glucagon-like peptide-1 receptor (GLP-1R) is a major therapeutic target for type 2 diabetes and obesity. Agonists showing bias in favour of G protein signalling over β-arrestin recruitment and GLP-1R internalisation, e.g ...
Hanh Duyen Tran, Yiming Zuo, Carissa Wong, Alice Pollard, Steve Bloom, Ben Jones   +5 more
doaj   +1 more source

The effect of arrestin conformation on the recruitment of c-Raf1, MEK1, and ERK1/2 activation.

PLoS ONE, 2011
Arrestins are multifunctional signaling adaptors originally discovered as proteins that "arrest" G protein activation by G protein-coupled receptors (GPCRs).
Sergio Coffa, Maya Breitman, Susan M Hanson, Kari Callaway, Seunghyi Kook, Kevin N Dalby, Vsevolod V Gurevich   +6 more
doaj   +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

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

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