Results 51 to 60 of about 149,829 (255)

Vitamin E Phosphate Nucleoside Prodrugs: A Platform for Intracellular Delivery of Monophosphorylated Nucleosides

Pharmaceuticals, 2018
Vitamin E phosphate (VEP) nucleoside prodrugs are designed to bypass two mechanisms of tumor resistance to therapeutic nucleosides: nucleoside transport and kinase downregulation.
Richard Daifuku, Michael Koratich, Murray Stackhouse   +2 more
doaj   +1 more source

Pyrazole‐Derived Antibacterial Compounds Effectively Treat Methicillin‐Resistant Staphylococcus Aureus Infections by Inhibiting Aspartate Transcarbamoylase

Advanced Science, EarlyView.
This study unveils a novel antibacterial mechanism against MRSA, in which the compound Py‐27 selectively targets and inhibits aspartate transcarbamoylase (ATCase), a key enzyme in pyrimidine synthesis. This inhibition disrupts DNA replication, induces oxidative damage, leading to potent bactericidal activity.
Xiaorong Yang, Xinyuan Cao, Lixia Dai, Feng Yang, Jing Wang, Yudong Ma, Tong Bu, Zile Gong, Xueyan Liu, Changcai Bai, Xiaolou Miao, Xiaofei Shang   +11 more
wiley   +1 more source

Construction of an Isonucleoside on a 2,6-Dioxobicyclo[3.2.0]-heptane Skeleton

Molecules, 2015
We have built a new isonucleoside derivative on a 2,6-dioxobicyclo[3.2.0]heptane skeleton as a potential anti-HIV agent. To synthesize the target compound, an acetal-protected dihydroxyacetone was first converted to a 2,3-epoxy-tetrahydrofuran ...
Yuichi Yoshimura, Satoshi Kobayashi, Hitomi Kaneko, Takeshi Suzuki, Tomozumi Imamichi   +4 more
doaj   +1 more source

Unveiling the Taxonomic Diversity and Unprecedented Biosynthetic Treasure of the Phylum Myxococcota

Advanced Science, EarlyView.
Natural products remain vital sources of therapeutics, and the phylum Myxococcota constitutes an especially rich reservoir for them. Based on decades of microbiological efforts, we present 154 new Myxococcota genomes and revise taxonomy quadrupling the number of families and genera.
Amay Ajaykumar Agrawal, Ronald Garcia, Guangyi Chen, Chantal D. Bader, Peter Sullivan, Alexander Popoff, Daniel Krug, Maja Hunter, Sebastian Walesch, Emilia Oueis, Christine Frank, Haowen Zhao, Joachim J. Hug, Sebastian Keller, Pascal Hirsch, Azat Tagirdzhanov, Tatiana Malygina, Mary Victory E. Gutierrez, Alexey Gurevich, Judith Boldt, Boyke Bunk, Jörg Overmann, Ulrich Nübel, Andreas Keller, Olga V. Kalinina, Rolf Müller   +25 more
wiley   +1 more source

Functional Characterization of the Saccharomyces cerevisiae Equilibrative Nucleoside Transporter 1 (ScENT1)

Molecules, 2018
Equilibrative nucleoside transporters (ENTs) are polytopic membrane transporters responsible for the translocation of nucleosides, nucleobases—to a lesser extent—and nucleoside analog therapeutics across cellular membranes.
Rebba C. Boswell-Casteel, Jennifer M. Johnson, Franklin A. Hays   +2 more
doaj   +1 more source

Fibrillarin Resists Cellular Senescence Via SIRT1‐Dependent Nicotinamide Metabolism and Its Inhibition Sensitizes Senolytic Therapy in Esophageal Squamous Cell Carcinoma

Advanced Science, EarlyView.
FBL directly binds to and stabilizes SIRT1 by blocking its ubiquitin‐proteasome degradation, thereby sustaining nicotinamide metabolism and redox homeostasis to counteract cellular senescence in ESCC. Genetic and pharmacological suppression of FBL sensitizes tumor cells to senolytic therapy.
Xing Jin, Hong Liu, Ling Gao, Lei Liu, Ji‐Bin Liu, Xiaoxia Jin, Ming‐Song Wang, Dan Liu, Li Feng, Wen‐Lian Chen   +9 more
wiley   +1 more source

A C‐Nucleoside Analogue of Cordycepin With High Metabolic Stability and Potent Anti‐Psoriatic Activity via Microneedle Delivery

Advanced Science, EarlyView.
This work identified CPD3a as a potent, stable C‐nucleoside cordycepin derivative. When formulated into microneedle array for topical treatment, it ameliorated psoriasis by rebalancing immunity and enhancing antioxidant defenses. ABSTRACT Psoriasis is a chronic inflammatory disorder characterized by immune dysregulation and epidermal hyperplasia ...
Wenfang Pan, Xinyue Shao, Yuanchen Zhong, Xujie Sun, Lixuan Yin, Zongyan He, Tianqun Lang, Yuanchao Xie   +7 more
wiley   +1 more source

Nucleoside‐Modified mRNA Encoding Alpha‐Galactosidase A Ameliorates Fabry Disease Phenotypes in Human IPSC‐Derived Cardiomyocytes

Advanced Science, EarlyView.
Human iPSC‐derived Fabry cardiomyocytes exhibited broad transcriptional dysregulation, apoptosis, mitochondrial dysfunction, impaired reactive oxygen species handling, altered contractility, and abnormal calcium transient decay, potentially mediated by phospholamban hyperphosphorylation.
Malte Juchem, Lea Oehlsen, Sedef Ersoy, Jia Li Ye, Natalie Weber, Elisa Mohr, Wilson Agyapong, Junqing Liu, Maximilian Fuchs, Ke Xiao, Christopher Jahn, Reto Eggenschwiler, Tobias Cantz, Julia Beimdiek, Falk F. R. Buettner, Theresia Kraft, Jan Hegermann, Ivonne J. Knorr, Lisa Ernst, Linda Feldbrügge, Resa Puffert, Kevin Schmidt, Christian Bär, Jeannine Hoepfner, Thomas Thum   +24 more
wiley   +1 more source

Supramolecular Degraders: An Emerging Paradigm in Targeted Protein Degradation

Advanced Science, EarlyView.
Dynamic supramolecular assembly reshapes targeted protein degradation by coordinating modular degrader construction, delivery, functional integration, and intracellular assembly or activation across proteasomal, endosomal–lysosomal, and autophagy–lysosomal pathways.
Kongjun Liu, Xue Yuan, Yan Zhou, Rui Yuan, Shaocheng Xie, Yong Chen, Peiyi Wang, Jianmei Gao, Qihai Gong   +8 more
wiley   +1 more source

AL398, A Novel NSUN6 Inhibitor, Attenuates Epithelial‐Mesenchymal Transition and Metastasis in Endometrial Cancer by Abrogating m5C‐Dependent Stabilization of Snail mRNA

Advanced Science, EarlyView.
Proposed molecular mechanism: NSUN6 catalyzes m5C methylation on Snail mRNA to enhance its stability, leading to Snail upregulation and EMT promotion. The first‐in‐class inhibitor AL398 suppresses endometrial cancer metastasis by targeting the NSUN6‐m5C‐Snail. axis. ABSTRACT Endometrial cancer (EC) constitutes a leading gynecologic malignancy for which
Xiangzhuan Zhao, Linlin Yang, Huanxiang Chen, Chenfeng Guo, Hongshen Lu, Ying Zhu, Xuanzhi Wang, Yang Li, Ruike Zhang, Zichong Huang, Yifang Chen, Keyu Jin, Zeduo Xu, Lingxiu Meng, Longfeng Zhang, Yuanyuan Han, Yicong Yan, Qiaozhen Kang, Junhu Wan, Hongyang Liu   +19 more
wiley   +1 more source