Results 271 to 280 of about 130,472 (328)

Allosteric Regulation of Ectopically Expressed Olfactory Receptors in Tumor Cells: Ligand-Receptor Topology and Deep Learning-Assisted Drug Discovery [PDF]

Sandeep Bansal, Saanvi Gudisay
openalex   +1 more source

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

Allosteric regulation of pyruvate kinase enables efficient and robust gluconeogenesis by preventing metabolic conflicts and carbon overflow. [PDF]

mSystems
She F, Anderson BW, Khana DB, Zhang S, Steinchen W, Fung DK, Lesser NG, Lucas LN, Stevenson DM, Astmann TJ, Bange G, van Pijkeren J-P, Amador-Noguez D, Wang JD.   +13 more
europepmc   +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

Structural basis of the allosteric regulation of cyanobacterial glucose-6-phosphate dehydrogenase by the redox sensor OpcA. [PDF]

Proc Natl Acad Sci U S A
Doello S, Shvarev D, Theune M, Sauerwein J, Klon A, Keskin E, Boehm M, Gutekunst K, Forchhammer K.   +8 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

Cooperative Substructure and Energetics of Allosteric Regulation of the Catalytic Core of the E3 Ubiquitin Ligase Parkin by Phosphorylated Ubiquitin. [PDF]

Biomolecules
Ye X, Kotaru S, Lopes R, Cravens S, Lasagna M, Wand AJ.   +5 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

The mechanism of allosteric regulation of calcium-independent phospholipase A₂ by ATP and calmodulin binding to the ankyrin domain. [PDF]

Proc Natl Acad Sci U S A
Mouchlis VD, Hsu YH, Hayashi D, Cao J, Li S, McCammon JA, Dennis EA.   +6 more
europepmc   +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