Results 81 to 90 of about 7,863 (172)

Activation of peripheral NOP receptors reduces periorbital mechanical allodynia evoked by CGRP in mice

British Journal of Pharmacology, EarlyView.
Background and Purpose Migraine is a neurovascular disorder largely mediated by calcitonin gene‐related peptide (CGRP). This study explores the role of the nociceptin/orphanin FQ (N/OFQ)–N/OFQ receptor (NOP) system in CGRP‐induced periorbital mechanical allodynia (PMA) in mice.
Chiara Sturaro, Pietro Pola, Michela Argentieri, Alessia Frezza, Matilde Marini, Francesco De Logu, Valentina Albanese, Marie Soukupova, Davide Malfacini, Nurulain T. Zaveri, Romina Nassini, Dane D. Jensen, Pierangelo Geppetti, Girolamo Calò, Chiara Ruzza   +14 more
wiley   +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

Targeting KRAS for cancer therapy

British Journal of Pharmacology, EarlyView.
In recent years, therapeutics targeted against KRAS proto‐oncogene GTPase (KRAS)‐mutant cancers have seen significant progress. Herein we outline the biology and epidemiology of KRAS alterations at the lineage and allele levels, reviewing the clinical evidence for KRASG12C inhibition from the discovery of the recessive switch pocket to sotorasib ...
Jianlong Jia, Ruonan Liu, Tonia A. Adamide, Isis E. Fernandez, Georgios T. Stathopoulos   +4 more
wiley   +1 more source

Red fluorescent protein-aequorin fusions as improved bioluminescent Ca2+ reporters in single cells and mice.

PLoS ONE, 2011
Bioluminescence recording of Ca(2+) signals with the photoprotein aequorin does not require radiative energy input and can be measured with a low background and good temporal resolution.
Adil Bakayan, Cecilia F Vaquero, Fernando Picazo, Juan Llopis   +3 more
doaj   +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

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

British Journal of Pharmacology, Volume 183, Issue 17, Page 5315-5335, September 2026.
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, Joshua Richard, Suvankar Ghosh, Jillian Jerwick, Joice T. Gavali, Raymond B. Penn, Alexander D. MacKerell Jr, Deepak A. Deshpande   +7 more
wiley   +1 more source

Genetically encoded fluorogenic RNA-based bioluminescence resonance energy transfer (BRET) sensors for cellular imaging and target detection

SLAS Discovery
Fluorescence- and bioluminescence-based probes are valuable tools for understanding cell functions in health and disease. Bioluminescence offers an ideal complementary readout to fluorescence due to its minimal background interference and self ...
Lan Mi, Mingxu You
doaj   +1 more source

The selective degradation of PDE4B shortform, using a PROTAC, leads to inhibition of several hallmarks of cancer in HCT116 cells

British Journal of Pharmacology, Volume 183, Issue 18, Page 5516-5540, September 2026.
Background and Purpose Colorectal cancer is one of the most prevalent cancers worldwide, and novel precision medicine approaches are rapidly improving patient outcomes. Phosphodiesterase 4B (PDE4B) is a member of an enzyme family (PDE4) that hydrolyses intracellular cAMP to control spatial and temporal signalling cues.
Alina Zorn, John Daniel Pediani, Madihah Hussain, Jiayue Ling, Elaine Brown, Igor Belka, Eduardo Torres, Cathy Swindlehurst, Kyle Chan, David Stirling, George S. Baillie, Yuan Yan Sin   +11 more
wiley   +1 more source

Ratiometric Zinc Biosensor Based on Bioluminescence Resonance Energy Transfer: Trace Metal Ion Determination with Tunable Response. [PDF]

Int J Mol Sci, 2022
Matveeva EG, Stoddard AK, Zeng HH, Franke G, Bourne L, Fierke CA, Thompson RB.   +6 more
europepmc   +1 more source

Applications of bioluminescence-mediated photodynamic therapy (BL-PDT) for the treatment of deep-seated tumours

Discover Oncology
Bioluminescence, the light generated through biochemical reactions involving luciferases in living organisms, has been the focus of extensive research due to its diverse applications.
Mpho Mohlongo, Blassan P. George, Heidi Abrahamse   +2 more
doaj   +1 more source