Results 141 to 150 of about 32,685 (264)
Dualsteric and dual‐acting modulation of muscarinic receptors by antagonist KH‐5
Abstract Background and purpose Muscarinic acetylcholine receptors are key therapeutic targets, and ligands engaging both orthosteric and allosteric sites may offer improved selectivity and efficacy. Here, we investigated whether the muscarinic antagonist KH‐5 acts as a dualsteric antagonist and defined its mode of interaction with muscarinic receptors.
Alena Janoušková‐Randáková +3 more
wiley +1 more source
METTL18 is Required for Developmental, Metabolic, and Endocrine Regulation of Mammalian Growth
METTL18 is essential for histidine Nτ‐methylation of proteins, normal embryonic development, iron and lipid metabolism, and hormone signaling pathways that support postnatal growth in mice. The main points of this study are as follows: First, mouse METTL18 catalyzes histidine Nτ‐methylation. Next, Mettl18 KO embryos are significantly smaller than their
Fumiya Kasai +16 more
wiley +1 more source
BRET‐Based Approaches for Ion Channels: Emerging Applications and Future Directions
Bioluminescence resonance energy transfer (BRET) is a versatile method for studying ligand–protein interactions. Its compatibility with high‐throughput screening and real‐time kinetics has made it widely used in drug discovery. Here, we summarize recent applications of BRET‐based methods for studying ligand binding to ion channels, highlighting key ...
Nadine Kock +6 more
wiley +1 more source
TH Nguyen Pham,1 Nigel A Lengkeek,2 Ivan Greguric,2 Byung J Kim,1 Paul A Pellegrini,2 Stephanie A Bickley,3 Marcel R Tanudji,3 Stephen K Jones,3 Brian S Hawkett,1 Binh TT Pham1 1Key Centre for Polymers and Colloids, School of Chemistry, University of ...
Pham THN +9 more
doaj
Celebration of the 13th ICCNS meeting joint to the 1st ARBIOCOM Conference held on the site of Nice in December 2025. Abstract The 13th International Workshop on the CCN Family of Genes, held in Nice as part of the inaugural ARBIOCOM World Conference, brought together investigators with diverse research backgrounds, disciplines, and expertise. Building
Bernard Perbal +3 more
wiley +1 more source
Abstract Remlifanserin (ACP‐204) is a selective 5‐HT2A receptor inverse agonist that builds upon scientific findings of its structural analog, pimavanserin. This Phase 1, open‐label study in healthy adults (N = 16) describes the central 5‐HT2A receptor occupancy of remlifanserin at different doses and plasma concentrations using positron emission ...
Ethan S. Burstein +9 more
wiley +1 more source
Antibody–drug conjugates (ADCs) combine the specificity of an antibody with the potency of a cytotoxic drug. Thirteen ADCs, utilizing seven unique cytotoxic payloads and targeting 11 distinct antigens, are currently approved by the US Food and Drug Administration as of June 2025, representing a rapidly growing and highly promising class of anticancer ...
Sijie Lu +6 more
wiley +1 more source
TRENDS IN RADIOISOTOPES AND RADIOLABELING METHODS
Summary: Radiopharmaceutical research and bioscience or medical applications have changed during the decades in the function of available technologies for radioisotope production and imaging detection technologies.
Fabio Luiz Navarro MARQUES
core +1 more source
Nanomaterials integrate radiotherapy and immunotherapy by enhancing radiosensitivity, remodeling the immunosuppressive tumor microenvironment, and promoting systemic antitumor immunity. This review summarizes the latest strategies of nanomaterial‐mediated combinations (RT, immunotherapy, IRT) and highlights future directions for overcoming clinical ...
Peijie Li, Xiangqin Wang, Sisi He, Hu Ma
wiley +1 more source
The image illustrates how PROTACs utilize endocytosis, mediated by cell surface proteins, to overcome bioavailability limitations and enable efficient intracellular delivery. ABSTRACT Proteolysis‐targeting chimeras (PROTACs) are promising therapeutic agents for targeted protein degradation via the ubiquitin‐proteasome system; however, their clinical ...
Huahua Chen +3 more
wiley +1 more source

