Results 141 to 150 of about 67,843 (252)

Peripheral targets for neuropathic pain

British Journal of Pharmacology, EarlyView.
Neuropathic pain represents a significant clinical challenge, with still limited pharmacological approaches to symptomatic relief. This review focuses on molecular targets implicated in neuropathic pain, particularly those involved in peripheral mechanisms. Using the IUPHAR/BPS database of biological targets, their occurrence together with ‘neuropathic
Amirhossein Afsharipour, Cosmin I. Ciotu, Felix J. Resch, Michael J. M. Fischer   +3 more
wiley   +1 more source

Systematic profiling reveals broad G protein coupling and context‐dependent modulation of cyclic AMP by the orphan receptor GPR139

British Journal of Pharmacology, EarlyView.
Background and Purpose G protein‐coupled receptors (GPCRs) are major drug targets, yet many orphan receptors remain poorly characterized. GPR139 has been implicated in CNS disorders, including schizophrenia and depression, but its signalling mechanisms remain unclear.
Boris Trapkov, Hans Bräuner, Alexander Sebastian Hauser   +2 more
wiley   +1 more source

Signal detection and characterisation of a novel drug–drug interaction between methadone and a synthetic cannabinoid receptor agonist

British Journal of Pharmacology, EarlyView.
Background and Purpose Little is known about how synthetic cannabinoid receptor agonist (SCRA) co‐use with other psychoactive substances may exacerbate risk of death. This study aimed to characterise the polypharmacy of deaths where SCRAs were detected at post‐mortem, investigate the cardiotoxicity of SCRAs and probe their inhibition of human ether‐a ...
Kirsten L. Rock, Louise M. Hesketh, Hongwei Cheng, Shuoqi Chen, Simon Hudson, Graeme Henderson, Jules C. Hancox, Michael J. Shattock, Michael J. Curtis, Caroline S. Copeland   +9 more
wiley   +1 more source

Residue Interaction Network Reveals Allosteric Pathways Linking Orthosteric and Intracellular Sites in Class A GPCRs. [PDF]

J Chem Inf Model
Peter S, Chalhoub G, McCormick PJ, De Graaf C, Chen I, Bottegoni G.   +5 more
europepmc   +1 more source

The c‐Src inhibitor eCF506 diminishes opioid tolerance and reduces β‐arrestin2 recruitment

British Journal of Pharmacology, EarlyView.
Morphine activation of μ receptors causes tolerance through c‐Src activation and β‐arrestin2 recruitment. c‐Src inhibition or degradation reduces β‐arrestin2 recruitment, μ receptor endocytosis, while causing receptor upregulation, all likely contributing to reduced morphine tolerance.
Samuel Singleton, Fraser Nunn, Erika Lace, Álvaro Lorente‐Macías, Rachel Toth, Asier Unciti‐Broceta, Tim G. Hales   +6 more
wiley   +1 more source

Decoding GPCR signaling in living cells to advance early therapeutic discovery for neurological disorders. [PDF]

Front Mol Neurosci
Palladino G, Patarra R, Li Z, Rossner MJ, Wehr MC.   +4 more
europepmc   +1 more source

Positive modulation of glucagon‐like peptide 1 (GLP‐1) receptor by endogenous haemorphins with implications in glucose metabolism and diabetes

British Journal of Pharmacology, EarlyView.
Haemorphins act on GLP‐1 receptor (GLP‐1R) activity and signalling in a positive allosteric manner. This leads to potentiated GLP‐1‐mediated activity and signalling, as well as insulin synthesis, which may have implications for glucose metabolism and, thereby, diabetes and obesity. (The graph was created in BioRender.com).
Farheen Badrealam Khan, Rwdah Mohamed Alameri, Yasir S. Raouf, Damien Maurel, Naiem Ahmad Wani, Anatoliy Shmygol, Irfa Anwar, Heng B. See, Elizabeth K. M. Johnstone, Elodie Dupuis, Eric Trinquet, Kevin D. G. Pfleger, Emilia Oueis, Mohammed Akli Ayoub   +13 more
wiley   +1 more source

pH sensing and inflammation: linking acidic microenvironments to immune reprogramming. [PDF]

Front Immunol
Zhang M, Tian J, Sun W.
europepmc   +1 more source

GPCR biosensor chip [PDF]

Nature Biotechnology, 1999
openaire   +2 more sources

GPCRs interaction with LGR5: Implications to cancer stemness. [PDF]

J Cancer
Nag JK, Subedi G, Rudina T, Bar-Shavit R.   +3 more
europepmc   +1 more source