Results 181 to 190 of about 19,325 (262)

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

ENX-101, a GABA_A receptor α2,3,5-selective positive allosteric modulator, displays antiseizure effects in rodent seizure and epilepsy models. [PDF]

Epilepsia
Serrats J, Vadodaria KC, Brubaker W, Barker-Haliski M, White HS, Evrard A, Roucard C, Taylor E, Vanover KE, Cunningham S, Sudarsan V, Rogawski MA.   +11 more
europepmc   +1 more source

Targeting protein–protein interactions with reversible covalent modalities: Non‐cysteine chemistries

British Journal of Pharmacology, EarlyView.
Abstract Protein–protein interactions (PPIs) are central to diverse cellular functions, and represent a rapidly expanding class of therapeutic targets. Advancements in covalent drug design have enabled small‐molecule drugs to overcome challenges associated with engaging these targets, such as limited durations of action and difficult‐to‐drug (expansive,
Ruchira Basu, Steven Fletcher
wiley   +1 more source

Gut microbe-generated phenylacetylglutamine is an endogenous allosteric modulator of β2-adrenergic receptors. [PDF]

Nat Commun
Saha PP, Gogonea V, Sweet W, Mohan ML, Singh KD, Anderson JT, Mallela D, Witherow C, Kar N, Stenson K, Harford T, Fischbach MA, Brown JM, Karnik SS, Moravec CS, DiDonato JA, Naga Prasad SV, Hazen SL.   +17 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

Safety, tolerability, pharmacokinetic and pharmacodynamic effects of the muscarinic M₁ positive allosteric modulator VU0467319 for Alzheimer's disease: a single ascending-dose study in healthy participants. [PDF]

Alzheimers Res Ther
Conley AC, Key AP, Blackford JU, Russell JK, Albert KM, Gong X, Bubser M, Rook JM, Conn PJ, Lindsley CW, Jones CK, Newhouse PA.   +11 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

Roles of ER Membrane Protein Complex in Protein Biogenesis and Quality Control in the Lung and Beyond

Cell Proliferation, EarlyView.
The endoplasmic reticulum membrane protein complex (EMC) is an evolutionarily conserved, multi‐subunit transmembrane protein complex crucial to membrane protein biogenesis and cellular protein quality control. This review systematically examines the structure, functions and disease‐associated regulatory mechanisms of EMC across multiple organ systems ...
Yan Qiao, Yuqing Sun, Yutao Huang, Qinghang Meng, Xinhua Lin, Wei Wei, Xiaofang Tang   +6 more
wiley   +1 more source

Structure-based identification of a G protein-biased allosteric modulator of cannabinoid receptor CB1. [PDF]

Proc Natl Acad Sci U S A
Shen S, Wu C, Lin G, Yang X, Zhou Y, Zhao C, Miao Z, Tian X, Wang K, Yang Z, Liu Z, Guo N, Li Y, Xia A, Zhou P, Liu J, Yan W, Ke B, Yang S, Shao Z.   +19 more
europepmc   +1 more source