Results 191 to 200 of about 31,985 (308)

Comprehensive transduceromic profiling of NOP receptor ligands at different Gα subunits

British Journal of Pharmacology, EarlyView.
Abstract Background and Purpose The nociceptin/orphanin FQ (N/OFQ) peptide receptor (NOP) is an opioid receptor family member with distinct pharmacology and broad therapeutic potential. NOP receptors regulate functions such as nociception, stress reactivity, reward, mood, autonomic tone, immunity and sleep/wake cycle.
Davide Malfacini, Riccardo Camilotto, Michele Maritan, Erika Morrone, Stephen Afriyie Boateng, Anna Vacilotto, Salvatore Pacifico, Remo Guerrini, Nurulain T. Zaveri, Girolamo Calo'   +9 more
wiley   +1 more source

Opening closed inward rectifier potassium channel doors

British Journal of Pharmacology, EarlyView.
Inwardly rectifying potassium (KIR) channels are essential regulators of membrane potential in excitable and non‐excitable tissues. Although KIR channels exhibit a biophysical preference for potassium influx due to voltage‐dependent block of outward current by polyamines and Mg2+, under physiological conditions, they predominantly mediate K+ efflux ...
Anna Stary‐Weinzinger, Fabian Kaiser, Marcel A. G. van der Heyden, Saïd Bendahhou   +3 more
wiley   +1 more source

Application of Deuterium in an M₁ Positive Allosteric Modulator Back-Up Program: The Discovery of VU6045422. [PDF]

ACS Chem Neurosci
Engers JL, Li J, Han C, Long MF, Gregro AR, Presley CC, Dickerson JW, Peng W, Cho HP, Rodriguez AL, Xiang Z, Boutaud O, O'Carroll C, Dey PM, Burstein ES, Niswender CM, Rook JM, Conn PJ, Engers DW, Lindsley CW.   +19 more
europepmc   +1 more source

Novel drugs approved by the EMA, the FDA and the MHRA in 2025: A year in review

British Journal of Pharmacology, EarlyView.
Abstract In the 2025 novel drug mini‐review, one can take a full measure of the ingenuity that underlies current drug design and development, despite the year's smaller harvest (46 novel drugs) compared to 2024 (53) and 2023 (70). 54% of the novel drugs are first‐in‐class (FIC).
Andreas Papapetropoulos, Stavros Topouzis, Steve P. H. Alexander, Miriam M. Cortese‐Krott, Zsuzsanna Helyes, Kirill Martemyanov, Claudio Mauro, Nithyanandan Nagercoil, Reynold A. Panettieri Jr, Hemal H. Patel, Rainer Schulz, Barbara Stefanska, Gary J. Stephens, Nathalie Vergnolle, Xin Wang, Stephen Ward, Péter Ferdinandy   +16 more
wiley   +1 more source

A Positive Allosteric Modulator of the SERCA Pump Rescues Hippocampal Neuronal Circuits Dysfunction and Cognitive Defects in a Mouse Model of Alzheimer's Disease. [PDF]

J Neurosci
Gerasimov E, Rakovskaya A, Pchitskaya E, Vlasova O, Dahl R, Bezprozvanny I.   +5 more
europepmc   +1 more source

Positive Allosteric Modulator of SERCA Pump NDC-1173 Exerts Beneficial Effects in Mouse Model of Alzheimer's Disease. [PDF]

Int J Mol Sci, 2023
Dahl R, Moore AC, Knight C, Mauger C, Zhang H, Schiltz GE, Koss WA, Bezprozvanny I.   +7 more
europepmc   +1 more source

Cannabidiol and cannabigerol ameliorate steatotic liver disease via phosphocreatine buffering and lysosomal restoration

British Journal of Pharmacology, EarlyView.
Cannabidiol (CBD) and cannabigerol (CBG) alleviate hepatic steatosis in obese mice by shifting energy buffering towards phosphocreatine and enhancing lysosomal lipid degradation and trafficking. These effects are associated with increased creatine kinase activity and lysobisphosphatidic acid (LBPA) levels, highlighting a previously unrecognised ...
Radka Kočvarová, Shahar Azar, Bella Agranovich, Ifat Abramovich, Saveliy Kirillov, Alina Nemirovski, Saja Baraghithy, Inbar Plaschkes, Emmanuelle Merquiol, Alexander Rouvinski, Galia Blum, Liad Hinden, Joseph Tam   +12 more
wiley   +1 more source

Formulation and characterization of CMPI nanoparticles for enhanced targeting of brain nicotinic receptors by positive allosteric modulator. [PDF]

Sci Rep
Aly R, Sulthana S, Beaudoin R, Hamouda AK, Aryal S.   +4 more
europepmc   +1 more source

Second‐generation prokineticin PKR1 receptor agonists: Advancing cardioprotection against chemotherapy‐induced toxicity

British Journal of Pharmacology, EarlyView.
IS39, a novel non‐peptide PKR1 agonist, confers cardioprotection against doxorubicin‐induced toxicity. IS39 activates PKR1‐mediated pro‐survival signalling in cardiomyocytes, reducing reactive oxygen species (ROS), DNA damage and fibrosis markers. In vivo, IS39 preserves cardiac geometry and function in mice exposed to chronic doxorubicin challenge ...
Anais Audebrand, Simone Brogi, Mustafa Tezeren, Andrea Tafi, Omer H. Ocak, Hasan Koyuncu, Igor Tetko, Laurent Désaubry, Canan G. Nebigil   +8 more
wiley   +1 more source

Clinical Applications of Phosphoproteomics: Illuminating Cancer Signaling and Enabling Rational Therapeutic Strategies

Cancer Science, EarlyView.
Mass spectrometry‐based phosphoproteomics for mechanistic dissection of cancer signaling pathways and uncovering therapeutic vulnerabilities. ABSTRACT Protein phosphorylation is a central post‐translational modification regulating cellular signaling, frequently dysregulated in cancer.
Hirokazu Shoji, Narikazu Boku, Jun Adachi   +2 more
wiley   +1 more source