Results 171 to 180 of about 13,822,676 (240)

Hippo Pathway–YAP/TAZ Signaling: Molecular Mechanisms, Biological Function, Diseases, and Therapeutic Targets

MedComm, Volume 7, Issue 10, October 2026.
The Hippo–YAP/TAZ–TEAD pathway integrates mechanical and biochemical cues to govern organ growth, regeneration, cancer, and fibrosis. This review dissects pathway physiology, TEAD structural pharmacology and ligandable pockets, and therapeutic strategies spanning palmitoylation‐pocket inhibitors, PROTAC degraders, and gene/RNA therapies, highlighting ...
Xiaodan Qu, Zhan‐you Wang
wiley   +1 more source

Naltrexone, Naloxone, Morphine, and Fentanyl Pharmacologically Chaperone a Mutant μ‐Opioid Receptor via an Endoplasmic Reticulum Exit Site‐Dependent Pathway

Pharmacology Research &Perspectives, Volume 14, Issue 5, October 2026.
ABSTRACT Opioid receptor antagonists increase the plasma membrane density of μ‐opioid receptors (MOR) in vivo, thereby inducing “supersensitivity” to opioid agonists. This phenomenon increases the risk of overdose in patients that were being treated with naltrexone (Ntx), a popular MOR antagonist.
Stephen N. Grant, Matthew J. Mulcahy, Henry A. Lester   +2 more
wiley   +1 more source

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

De Novo Discovery of Bioactive Cyclic Peptides via Cellular Selection of Genetically Encoded Libraries

ChemBioChem, Volume 27, Issue 18, 28 September 2026.
Genetically encoded cyclic peptide libraries can be employed in cellular selection platforms to identify cyclic peptide inhibitors for therapeutic targets by directly selecting for desired biological activities. This review systematically summarizes representative studies and suggests future opportunities for using cellular selection for de novo cyclic
Linwei Yang, Abhijit Behera, Hannah J. Meyers, Tina Wang   +3 more
wiley   +1 more source

Discovery of a Reversible Sub‐Picomolar Thrombin Inhibitor Using DCC

Angewandte Chemie, Volume 138, Issue 38, 14 September 2026.
An ultrapotent yet fully reversible trivalent thrombin inhibitor discovered through screening a large dynamic combinatorial library (DCL) of 125 000 members of self‐assembled fragments. The innovative approach leverages size‐exclusion‐based affinity selection, coupled with MALDI‐TOF mass spectrometry readout, enabling the full workflow to be completed ...
Millicent Dockerill, Richard J. Payne, Nicolas Winssinger   +2 more
wiley   +2 more sources

Organelle‐Resolved Tetrazine‐trans‐Cyclooctene Click Chemistry for Cargo Delivery and Release

Chemistry – A European Journal, Volume 32, Issue 35, 19 September 2026.
Bioorthogonal click chemistry tools provide a means for specific intracellular conjugation of molecules. In this study, we used reactive tetrazine (Tz) and TCO moieties for labeling of organelles and organelle‐specific delivery and activation of doxorubicin prodrugs.
Oleh Durydivka, Marek Chovanec, Rastislav Dzijak, Michal Rahm, Jachym Hrusak, Paul E. Reyes‐Gutierrez, Milan Vrabel   +6 more
wiley   +1 more source

Diarylethene‐Containing Photoswitchable Analogues of Tubulysins—Design, Synthesis, Biological, and Structural Evaluation

European Journal of Organic Chemistry, Volume 29, Issue 35, 19 September 2026.
Diarylethene‐containing cyclic tubulysin analogues were designed, synthesized, and evaluated as light‐responsive cytotoxic agents. One analogue showed reversible photoswitching, photoregulated tubulin polymerization inhibition, and photoform‐dependent cytotoxicity.
Anna Iampolska, Sergii Afonin, Oleg Babii, Mahri Park, Juan Estévez‐Gallego, Michel O. Steinmetz, Andrea E. Prota, Anne S. Ulrich, David R. Spring, Igor V. Komarov   +9 more
wiley   +1 more source

Borylcyclopropanes: Synthetic Strategies and Applications

Angewandte Chemie, Volume 138, Issue 37, 7 September 2026.
Borylcyclopropanes (cyclopropanes bearing a boron substituent) sit at the intersection of two privileged frameworks in synthesis. This review provides the first exhaustive survey of their chemistry, spanning metal–carbene, nucleophilic cyclization, radical, hydroboration, and C─H activation routes, and documenting applications in medicinal chemistry ...
Aiza A. Butt, Joseph M. Ready
wiley   +2 more sources

Discovery of novel acridine based inhibitors of Bruton's tyrosine kinase (BTK) via pharmacophore modeling and machine learning-driven virtual screening followed by molecular dynamic studies. [PDF]

J Comput Aided Mol Des
Shahin R, Jaafreh S, Mansi I, Al Zoubi R, Abu-Irmaileh B, Azzam Y, Azzam S.   +6 more
europepmc   +1 more source

Identification of novel PKR inhibitory chemotypes <i>via</i> integrated molecular modelling and machine learning. [PDF]

RSC Adv
Shakhatreh G, Taha MO, Daoud S.
europepmc   +1 more source