Results 101 to 110 of about 15,825 (259)

Progress on the development of Class A GPCR‐biased ligands

British Journal of Pharmacology, Volume 182, Issue 14, Page 3249-3300, July 2025.
Class A G protein‐coupled receptors (GPCRs) continue to garner interest for their essential roles in cell signalling and their importance as drug targets. Although numerous drugs in the clinic target these receptors, over 60% GPCRs remain unexploited. Moreover, the adverse effects triggered by the available unbiased GPCR modulators, limit their use and
Paula Morales, Magdalena M. Scharf, Marcel Bermudez, Attila Egyed, Rafael Franco, Olivia K. Hansen, Nadine Jagerovic, Jan Jakubík, György M. Keserű, Dóra Judit Kiss, Pawel Kozielewicz, Olav Larsen, Maria Majellaro, Ana Mallo‐Abreu, Gemma Navarro, Rubén Prieto‐Díaz, Mette M. Rosenkilde, Eddy Sotelo, Holger Stark, Tobias Werner, Laura M. Wingler   +20 more
wiley   +1 more source

Swimming against the tide: investigations of the C-Bouton synapse

Frontiers in Neural Circuits, 2014
C-boutons are important cholinergic modulatory loci for state-dependent alterations in motoneuron firing rate. Type 2 muscarinic acetylcholine (m2) receptors are concentrated postsynaptic to C-boutons, and m2 receptor activation increases motoneuron ...
Adam S. Deardorff, Shannon H. Romer, Patrick M. Sonner, Robert E.W. Fyffe   +3 more
doaj   +1 more source

Benzochalcogenodiazoles, Synthesis, and Applications in Medicinal Chemistry and Photomedicine

European Journal of Organic Chemistry, Volume 28, Issue 23, June 23, 2025.
Benzochalcogenodiazoles (BXD) including benzoxadiazoles, benzothiadiazoles, and benzoselenadiazoles are initially mainly designed for optoelectronic materials as electron‐deficient cores. Nevertheless, they are now extending their application to biology.
Jean‐Elie Zheng, Xavier Franck, Thibault Gallavardin   +2 more
wiley   +1 more source

Molecular Biological Mechanisms of Yuan Zhi Powder in the Treatment of Alzheimer’s Disease: an Analysis Based on Network Pharmacology

Digital Chinese Medicine, 2018
: Objective To predict the main active ingredients, potential targets and molecular mechanisms of Yuan Zhi powder in treatment of dementia by using network pharmacology.Methods A database of chemical constituents of Yuan Zhi powder was constructed by ...
Wei-Jie Qiang, Ying Chen, Fu-Yuan He, Mei-Feng Xiao, Wei-Yan Cai, Yi-Fei Dai, Qing Yang, Yu-Jie Li, Xiao-Gang Weng, Qi Li, Ya-Jie Wang, Xiao-Xin Zhu   +11 more
doaj  

Acetylcholine Release Inhibits Distinct Excitatory Inputs Onto Hippocampal CA1 Pyramidal Neurons via Different Cellular and Network Mechanisms

Frontiers in Cellular Neuroscience, 2019
In hippocampal CA1, muscarinic acetylcholine (ACh) receptor (mAChR) activation via exogenous application of cholinergic agonists has been shown to presynaptically inhibit Schaffer collateral (SC) glutamatergic inputs in stratum radiatum (SR), and ...
Priyodarshan Goswamee, A. Rory McQuiston
doaj   +1 more source

Mechanistic insights into allosteric structure-function relationships at the M1 muscarinic acetylcholine receptor [PDF]

, 2014
Background: Selective and potent positive allosteric modulators (PAMs) of the M1 mAChR have been recently described. Results: Use of structural analogues and mutagenic mapping identified the mechanistic basis for increased PAM activity.
Abdul-Ridha, Byun, Canals, Christopoulos, Conn, Conn, Dror, Foster, Haga, Hulme, Jones, Katritch, Kenakin, Kennedy, Keov, Kruse, Kruse, Kruse, Kuduk, Kuduk, Kuduk, Lazareno, Leach, Leach, Lebois, Lebon, Ma, Matsui, May, Melancon, Mistry, Motulsky, Nathan, Nawaratne, Nickols, Phillips, Ragnarsson, Shirey, Shonberg, Stevens, Tarr, Valant, Venkatakrishnan   +42 more
core   +2 more sources

Biomimetic Design of Biocompatible Neural Probes for Deep Brain Signal Monitoring and Stimulation: Super Static Interface for Immune Response‐Enhanced Contact

Advanced Functional Materials, Volume 35, Issue 23, June 5, 2025.
Ultrathin, flexible neural probes are developed with an innovative, biomimetic design incorporating brain tissue‐compatible materials. The material system employs biomolecule‐based encapsulation agents to mitigate inflammatory responses, as demonstrated through comprehensive in vitro and in vivo studies.
Jeonghwa Jeong, Gyeonghwa Heo, Young Woo Kwon, Seon Yeong Chae, Min Jae Kim, Ki Jun Yu, Hwa Kyoung Shin, Suck Won Hong   +7 more
wiley   +1 more source

Gut microbial bile acid metabolite skews macrophage polarization and contributes to high-fat diet-induced colonic inflammation

Gut Microbes, 2020
High-fat diet (HFD) leads to systemic low-grade inflammation, which has been involved in the pathogenesis of diverse metabolic and inflammatory diseases.
Lingyu Wang, Zizhen Gong, Xiuyuan Zhang, Fangxinxing Zhu, Yuchen Liu, Chaozhi Jin, Xixi Du, Congfeng Xu, Yingwei Chen, Wei Cai, Chunyan Tian, Jin Wu   +11 more
doaj   +1 more source

Molecular mechanisms for fetal cardiac arrhythmia in intrahepatic cholestasis of pregnancy

, 2010
Intrahepatic cholestasis in pregnancy (ICP) is characterized by raised serum bile acids which can cause fetal complications, including preterm labour and intrauterine death. The fetal death in ICP is not well understood. In this thesis, the mechanisms of
Sheikh Abdul Kadir, Siti Hamimah, Sheikh Abdul Kadir, Siti Hamimah   +1 more
core   +1 more source

Ligand-guided homology modeling drives identification of novel histamine H3 receptor ligands [PDF]

, 2019
In this study, we report a ligand-guided homology modeling approach allowing the analysis of relevant binding site residue conformations and the identification of two novel histamine H3 receptor ligands with binding affinity in the nanomolar range.
Hagenow, Stefanie, Schaller, David, Stark, Holger, Wolber, Gerhard   +3 more
core   +2 more sources