Results 61 to 70 of about 24,311 (208)

Asymmetric Recruitment of β-Arrestin1/2 by the Angiotensin II Type I and Prostaglandin F2α Receptor Dimer

open access: yesFrontiers in Endocrinology, 2019
Initially identified as monomers, G protein-coupled receptors (GPCRs) can also form functional homo- and heterodimers that act as distinct signaling hubs for cellular signal integration.
Dany Fillion   +5 more
doaj   +1 more source

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

open access: yesBritish 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   +7 more
wiley   +1 more source

Distinct and shared roles of β-arrestin-1 and β-arrestin-2 on the regulation of C3a receptor signaling in human mast cells. [PDF]

open access: yesPLoS ONE, 2011
The complement component C3a induces degranulation in human mast cells via the activation of cell surface G protein coupled receptors (GPCR; C3aR).
Arpana Vibhuti   +4 more
doaj   +1 more source

The nitty‐gritty of vascular permeability in cancer: targeting blood endothelium to control metastases

open access: yesBritish Journal of Pharmacology, EarlyView.
Blood vascular permeability is a hallmark of cancer and acts as an active driver of metastatic dissemination. Metastasis accounts for the vast majority of cancer deaths, yet most work has focussed on tumour‐intrinsic traits and angiogenesis, while the specific contribution of endothelial barrier regulation to intravasation and extravasation remains ...
Pierre Boucher   +6 more
wiley   +1 more source

Agonist‐specific conformational dynamics at the β2‐adrenoceptor dictate allosteric modulation of Gαs signalling and bronchodilation

open access: yesBritish Journal of Pharmacology, EarlyView.
Abstract Background and Purpose β2‐adrenoceptor (β2AR) agonists are the cornerstone of asthma therapy and promote bronchodilation through Gαs signalling in airway smooth muscle (ASM), but their efficacy is limited by β‐arrestin‐mediated β2AR desensitization.
Sushrut D. Shah   +7 more
wiley   +1 more source

In silico prediction of novel effective combinational treatment of chronic pain in individual patients: A joint white paper of the H2020 QSPainRelief consortium

open access: yesBritish Journal of Pharmacology, EarlyView.
Abstract Opioids are prescribed widely for chronic pain despite well‐recognised risks and variable long‐term benefit, reflecting the lack of effective alternatives for many patients. Combination therapies offer a promising strategy to enhance efficacy whilst reducing side effects.
André Mouraux   +26 more
wiley   +1 more source

Decoding functional specialization in G protein‐coupled receptors (GPCRs) through evolution‐guided residue profiling

open access: yesBritish Journal of Pharmacology, EarlyView.
Background and Purpose G protein‐coupled receptors (GPCRs) are integral membrane proteins that mediate physiological processes by enabling cells to detect and respond to diverse stimuli. Although many subfamily‐specific functional hotspots have been described, the family‐wide determinants of common and subfamily‐specific functions remain incomplete ...
Berkay Selçuk   +3 more
wiley   +1 more source

Peripheral κ opioid receptor in pain and inflammation: From molecular signalling and gene expression to drug discovery

open access: yesBritish Journal of Pharmacology, EarlyView.
The κ opioid receptor (κ receptor, KOR) is a G protein‐coupled receptor with well established roles in analgesia and immune modulation. Although historically studied primarily in the central nervous system (CNS), growing evidence indicates that κ signalling in peripheral tissues plays an important role in regulating pain, inflammation and immune ...
Rumsha Khan   +3 more
wiley   +1 more source

Peripheral targets for neuropathic pain

open access: yesBritish 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   +3 more
wiley   +1 more source

The chemokine receptor‐like fourth extracellular loop of the apelin receptor differentially regulates apelin and elabela binding and signalling

open access: yesBritish Journal of Pharmacology, EarlyView.
Abstract Background and Purpose Apelin and Elabela are endogenous ligands of the apelin receptor (apelin receptor/APJ), a GPCR involved in cardiovascular regulation and body fluid homeostasis. The human receptor contains a conserved disulfide bridge linking the N‐terminal domain to extracellular loop 3 (ECL3) via Cys19 and Cys281, forming a structural ...
Chloé Bonef   +11 more
wiley   +1 more source

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