Results 101 to 110 of about 27,334 (199)

Cross-communication between Gi and Gs in a G-protein-coupled receptor heterotetramer guided by a receptor C-terminal domain [PDF]

, 2018
BACKGROUND: G-protein-coupled receptor (GPCR) heteromeric complexes have distinct properties from homomeric GPCRs, giving rise to new receptor functionalities.
Aguinaga Andrés, David, Brugarolas Campillos, Marc, Canela Campos, Enric I., Casadó, Vicent, Cordomí, Arnau, Cortés Tejedor, Antonio, Ferré, Sergi, Franco Fernández, Rafael, Lluís i Biset, Carme, Mallol Montero, Josefa, McCormick, Peter J., Moreno Guillén, Estefanía, Navarro Brugal, Gemma, Pardo, Leonardo, Pérez-Benito, Laura   +14 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

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

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

Modelling the cAMP pathway using BioNessie, and the use of BVP techniques for solving ODEs (Poster Presentation) [PDF]

, 2007
Copyright @ 2007 Gu et al; licensee BioMed Central LtdBiochemists often conduct experiments in-vivo in order to explore observable behaviours and understand the dynamics of many intercellular and intracellular processes.
Bhalla S Upinder, David Gilbert, Des Higham, Houslay D Miles, Miles Houslay, Xu Gu   +5 more
core   +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

Non-Acidic Free Fatty Acid Receptor 4 Agonists with Antidiabetic Activity [PDF]

, 2016
The free fatty acid receptor 4 (FFA4 or GPR120) has appeared as an interesting potential target for the treatment of metabolic disorders. At present, most FFA4 ligands are carboxylic acids that are assumed to mimic the endogenous long-chain fatty acid ...
Azevedo, Carlos, Christiansen, Elisabeth, Dunlop, Julia, Hansen, Steffen, Hudson, Brian, Kępczyńska, Malgorzata A., Milligan, Graeme, Shumpukade, Bharat, Stocker, Claire J., Ulven, Trond, Wargent, Edward T., Watterson, Kenneth   +11 more
core   +3 more sources

Drugs that act on both G protein‐coupled receptors (GPCRs) and kinases: potentiation of effects, side effects and general aspects of drug pleiotropy

British Journal of Pharmacology, EarlyView.
Abstract Background A drug designed for a specific target often interacts with multiple targets, either unintentionally or as part of its intended mechanism of action. This has been called pharmacological pleiotropy or polypharmacology. There are key endogenous ligands such as ATP, GABA and glutamate that act on various proteins in humans. Furthermore,
Hampus Ljunggren, Aleksandr Sokolov, Flavio Ballante, Robert Fredriksson, Francisco Lagunas‐Rangel, Alexander S. Hauser, Stefan Knapp, Jörgen Jonsson, Helgi B. Schiöth   +8 more
wiley   +1 more source

Peri-operative opioid analgesia - when is enough too much? A review of opioid-induced tolerance and hyperalgesia [PDF]

, 2019
Opioids are a mainstay of acute pain management but can have many adverse effects, contributing to problematic long-term use. Opioid tolerance (increased dose needed for analgesia) and opioid-induced hyperalgesia (paradoxical increase in pain with opioid
Bull, Fiona, Colvin, Lesley, Hales, Tim
core   +2 more sources

GIP in Cardiovascular and Kidney Disease: From Physiology to Pharmacology

Diabetes, Obesity and Metabolism, EarlyView.
ABSTRACT Aims To provide a comprehensive overview of the cardiovascular and renal effects of glucose‐dependent insulinotropic polypeptide (GIP) by integrating its physiological role with recent human trial data on tirzepatide, the first dual GIP and glucagon‐like peptide‐1 (GLP‐1) receptor agonist.
Michelantonio De Fano, Line L. Haurum, Christine R. Schwarz, Francesca Porcellati, Andreas Andersen   +4 more
wiley   +1 more source