Results 101 to 110 of about 107,002 (300)

Inclusion of Enclosed Hydration Effects in the Binding Free Energy Estimation of Dopamine D3 Receptor Complexes

, 2019
Confined hydration and conformational flexibility are some of the challenges encountered for the rational design of selective antagonists of G-protein coupled receptors. We present a set of C3-substituted (-)-stepholidine derivatives as potent binders of
Cordone, Pierpaolo, Gadhiya, Satishkumar, Gallicchio, Emilio, Harding, Wayne W., Kurtzman, Tom, Pal, Rajat Kumar, Ramsey, Steve, Wickstrom, Lauren   +7 more
core   +2 more sources

Endogenous Ceramide 24:1 Constrains Th17‐Driven Neutrophilic Inflammation by Antagonizing EP2 Signaling

Advanced Science, EarlyView.
Cer24:1 levels are reduced in neutrophilic asthma and inversely correlate with disease severity and airway neutrophilia. Restoring Cer24:1 suppresses pathogenic Th17 differentiation by engaging EP2 on CD4+ T cells, thereby dampening the JAK2–STAT3–RORγt axis and reducing IL‐17 production.
Huan Liu, Abudureyimujiang Aili, Zheng Kuang, Liting Cao, Zemin Li, Ying Shang, Yingying Ge, Tingting Hu, Yongchang Sun, Wuli Zhao, Rong Jin, Chun Chang   +11 more
wiley   +1 more source

Propofol inhibits the voltage-gated sodium channel NaChBac at multiple sites. [PDF]

, 2018
Voltage-gated sodium (NaV) channels are important targets of general anesthetics, including the intravenous anesthetic propofol. Electrophysiology studies on the prokaryotic NaV channel NaChBac have demonstrated that propofol promotes channel activation ...
Bondarenko, Vasyl, Carnevale, Vincenzo, Covarrubias, Manuel, Dailey, William P., Eckenhoff, Roderic G., Granata, Daniele, Klein, Michael L., Tang, Pei, Wang, Yali, Wells, Marta M., Woll, Kellie, Xu, Yan, Yang, Elaine   +12 more
core   +1 more source

Nanoscale Spatial Organization of ARC High‐ and Low‐Order Assemblies at Excitatory Synapses

Advanced Science, EarlyView.
ARC (Activity‐Regulated Cytoskeleton‐Associated protein) mediates synaptic plasticity by forming nanoscale assemblies in neurons. Using super‐resolution microscopy and time‐resolved anisotropy with targeted tagging, the study reveals low‐order ARC assemblies at synapses colocalizing with AMPARs, semi‐circular structures at endocytic zones, and 60–80 nm
Martina Damenti, Giovanna Coceano, Mariline Mendes Silva, Jonatan Alvelid, Chiara Sgattoni, Andrea Volpato, Lea Rems, Luciano A. Masullo, Eduard M. Unterauer, Rafal Kowalewski, Lucie Delemotte, Erdinc Sezgin, Ralf Jungmann, Ilaria Testa   +13 more
wiley   +1 more source

The ITGB2‐COPS3‐SOX2 Axis and SOX2 Liquid‐Liquid Phase Separation: Dual Mechanisms Governing Osteosarcoma Stemness

Advanced Science, EarlyView.
Osteosarcoma stemness is driven by the ITGB2‐COPS3‐SOX2 signaling axis. This study reveals that nuclear COPS3 stabilizes SOX2, which in turn undergoes liquid‐liquid phase separation to promote stemness. Based on this mechanism, a novel COPS3 inhibitor, Z‐5891, was developed, effectively suppressing tumor growth and stemness in vivo, offering a ...
Lei Guo, Zhiqing Zhao, Wei Wang, Jianfang Niu, Bing Wang, Yunfei Lin, Wei Guo, Taiqiang Yan   +7 more
wiley   +1 more source

Connexin 43‐Enriched Vesicles Improve Synchronization in hiPSC‐Derived Cardiomyocytes

Advanced Science, EarlyView.
Plasma membrane‐derived Connectosomes enriched in connexin‐43 are produced from donor hiPSCs and applied to hiPSC‐derived cardiomyocytes (hiPSC‐CMs). Connexin‐43 channels on Connectosomes remain functional, strengthening intercellular electrochemical coupling and increasing network synchronization over time.
Nima Momtahan, Anna K. McClain, Andrea Trementozzi, Sogu Sohn, Lingxia Qiao, Chi Zhao, Padmini Rangamani, Jeanne C. Stachowiak, Janet Zoldan   +8 more
wiley   +1 more source

Network Pharmacology, Molecular Docking and Dynamics Simulation Reveal the Anti-Colitis Mechanism of Smilax glabra Roxb.

Clinical and Experimental Gastroenterology
Yuan Cui,1,2 Jingyi Hu,1 Yanan Li,1 Yiheng Tong,1 Hong Shen1 1Department of Gastroenterology, Jiangsu Province Hospital of Chinese Medicine, Affiliated Hospital of Nanjing University of Chinese Medicine, Nanjing, 210001, People’s Republic of China ...
Cui Y, Hu J, Li Y, Tong Y, Shen H
doaj  

Molecular docking and molecular dynamics study of 3-hydroxybutyrate with polymers for diabetic ketoacidosis-targeted molecularly imprinted polymers [PDF]

Journal of Pharmacy & Pharmacognosy Research
Context: Molecularly imprinted polymers (MIPs) are promising materials with tailored binding sites that can selectively recognize and bind target molecules.
Aiyi Asnawi, Ellin Febrina, Widhya Aligita, La Ode Aman, Fachrul Razi   +4 more
doaj   +1 more source

Hepatocyte BDNF Acts as a Novel Immune Checkpoint to Restrain TLR4‐Mediated Acute Hepatitis

Advanced Science, EarlyView.
This study identifies hepatocyte‐derived BDNF as an endogenous TLR4 antagonist that alleviates acute hepatitis. BDNF is downregulated in hepatocytes via REST‐mediated transcriptional repression during ALI/ALF. Mechanistically, BDNF binds to TLR4 on macrophages to suppress inflammation.
Weiwei Zhu, Yaqian Cui, Yongqiang Zhou, Yihui Zheng, Lijiang Huang, Leiming Jin, Qianhui Zhang, Pan Chen, Mengsha Lin, Jiaxi Ye, Yongqiang Xiong, Joo Young Huh, Xiang Hu, Xiaokun Li, Wu Luo, Guang Liang   +15 more
wiley   +1 more source

Catechol Derivative‐Based Bioadhesives: Molecular Design for Precision Medical Adhesion

Advanced Science, EarlyView.
This study utilizes tree‐inspired side‐chain engineering to graft five catechol derivatives onto PVA, systematically revealing how side‐chain length and substituents regulate adhesion and cohesion properties. Among them, the PVA‐CA patch demonstrates superior tissue adhesion, biocompatibility, and promotes regeneration, establishing a programmable ...
Xueyu Wang, Zixin Yang, Shan Wang, Weiwei Tan, Zhirui He, Qinyu Duan, Huanan Wang, Tao Chen, Shanshan Hu   +8 more
wiley   +1 more source