Results 181 to 190 of about 33,330 (276)

Dualsteric and dual‐acting modulation of muscarinic receptors by antagonist KH‐5

British Journal of Pharmacology, Volume 183, Issue 19, Page 5769-5790, October 2026.
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, Eva Dolejší, Nikolai Chetverikov, Jan Jakubík   +3 more
wiley   +1 more source

Fruquintinib: Mechanism of Action, Clinical, and Translational Science

Clinical and Translational Science, Volume 19, Issue 10, October 2026.
ABSTRACT Fruquintinib is a highly selective, oral inhibitor of all three vascular endothelial growth factor receptors (‐1, ‐2, and ‐3) that was approved, including in China, the United States, and the European Union, for the treatment of previously treated metastatic colorectal cancer (mCRC).
Xiaofei Zhou, Arvind Dasari, Jin Li, Caly Chien, Qi Dong, Lucy Chen, Lixian Dong, Neeraj Gupta   +7 more
wiley   +1 more source

The Role of torS and torT Transcription in Driving a Bet‐Hedging Strategy for Trimethylamine N‐Oxide Reductase Expression in Escherichia coli

Molecular Microbiology, Volume 126, Issue 4, Page 379-395, October 2026.
Low basal activity of divergent promoters driving transcription of the trimethylamine N‐oxide (TMAO) sensor TorT and kinase TorS is integral to an O2‐regulated bet‐hedging strategy for continued E. coli growth upon the onset of anaerobiosis. This, along with repression by IscR, promotes noise in the TorS to TorT ratio, which is critical for adaptation ...
Erin L. Mettert, Jeffrey N. Carey, Wilma Ross, Mark Goulian, Patricia J. Kiley   +4 more
wiley   +1 more source

Development of a Highly Effective Bifunctional Ligand 2E-C-NETA for Targeted Lu-177 Therapy: Synthesis, Radiolabeling, In Vitro Stability, and In Vivo Biodistribution. [PDF]

ChemMedChem
Chen Y, Lee Y, Kang CS, Ren S, Chen Y, Wang H, Bandara N, Rogers BE, Chong HS.   +8 more
europepmc   +1 more source

Palladium-103 as a Theranostic Auger Electron Emitter: From Cyclotron Production to Preclinical SPECT Evaluation in Murine and Canine Models. [PDF]

Pharmaceuticals (Basel)
Laouameria AN, Máthé D, Kubovje A, Vajdovich P, Balka G, Hunyadi M, Bergmann RK, Halldin C, Forgách L, Horváth I, Szigeti K, Psáder R, Zeevaart JR, Csige L, Szűcs Z.   +14 more
europepmc   +1 more source

Metabolic Glycoengineering Enables Fluorine-18 Radiolabeling of T Lymphocytes via Dual-Bioorthogonal Chemistry. [PDF]

Bioconjug Chem
Biti A, Centanni A, Imlimthan S, Harjunpää H, Sukhova A, Wiedmer SK, Fagerholm S, Sarparanta M.   +7 more
europepmc   +1 more source

Optimization of ⁶⁸Ga-lactosylated human serum albumin (LSA) for PET-based quantitative evaluation of hepatic functional reserve in liver fibrosis models. [PDF]

J Nanobiotechnology
Park B, Park JY, Pahk K, Kim JS, Joung C, Byun JW, Yoo RJ, Mun JS, Chae K, Jeong JM, Kim S, Paeng JC, Lee YS.   +12 more
europepmc   +1 more source

Stable Chelation of Zr-89 and Ac-225 with Dual Size-Selective Macrocyclic py₂-macrodipa for ²²⁵Ac/⁸⁹Zr Paired Theranostics. [PDF]

Inorg Chem
Chakraborty M, Lee KK, Hasson A, Kanagasundaram T, Fears A, Hu A, Wilson JJ, Thorek DLJ.   +7 more
europepmc   +1 more source

Chelator Free Radiolabeling and Preclinical Evaluation of η⁶-Arene Sandwich Complexes of Lenalidomide With Rhenium and Technetium-99m. [PDF]

Chembiochem
Nadeem Q, Battistin F, Valdés DH, Genady AR, Mendez LRS, Sadeghi S, Blacque O, Alberto R.   +7 more
europepmc   +1 more source