Results 41 to 50 of about 29,245 (221)

Molecular docking, QSAR, and ADME studies of some pyrrolo[1, 2-a] benzimidazole-based quinones as novel topoisomerase 2 beta (TOP2β) inhibitors

Chemical Physics Impact
In recent years, selective topoisomerase II inhibitors have drawn interest in the development of novel antitumor compounds to an extraordinary degree. As potent topoisomerase II inhibitors, pyrrolo[1, 2-a]-benzimidazole quinones with a 6-aziridinyl group
Rahul D. Jawarkar, Anam N. Khan, Dhanashri R. Bhagat, Pravin N. Khatale, Pramod V. Burakale, Saleemuddin Farooqui, Suraj N. Mali   +6 more
doaj   +1 more source

Immunosuppressive Drug Use in Limited Systemic Sclerosis: An International Survey

Arthritis Care &Research, EarlyView.
Objective Current guidelines recommend immunosuppressive treatment for diffuse cutaneous systemic sclerosis but are less clear on their use in limited cutaneous systemic sclerosis (lcSSc) in the absence of internal organ complications. We conducted an international survey to understand current immunosuppressive drug prescribing patterns in lcSSc ...
Sabrina Hoa, Yicheng Mu, Marie Hudson, Janet Pope   +3 more
wiley   +1 more source

Real‐World Safety and Effectiveness of JAK Inhibitors in Systemic Sclerosis: A Propensity‐Matched Study From the EUSTAR Cohort

Arthritis Care &Research, EarlyView.
Objective JAK inhibitors (JAKi) have shown promising effects in early‐phase studies of systemic sclerosis (SSc). We aimed to assess the safety and explore the effectiveness of JAKi compared to conventional immunosuppressants in SSc. Methods A longitudinal retrospective study of the European Scleroderma Trials and Research Group (EUSTAR) cohort was ...
Stefano Di Donato, Marie‐Elise Truchetet, Marco Minerba, Oliver Distler, Juan José Alegre Sancho, Yolanda Braun‐Moscovici, Christina Bergmann, Petros Sfikakis, Jeska K. de Vries‐Bouwstra, Murray Baron, Silvia Bellando‐Randone, Lorenzo Dagna, Christopher P. Denton, Madelon C. Vonk, Vanessa Smith, Ivan Castellvi, Gabriela Riemekasten, Andra Balanescu, Masataka Kuwana, Maria De Santis, Kamal Solanki, Anastas Batalov, Vahan Mukuchyan, Marco Matucci‐Cerinic, Yannick Allanore, Francesco Del Galdo, Michael Hughes, EUSTAR Collaborators   +27 more
wiley   +1 more source

Mitochondria and Neuromast Tagging With Fluorescent Gallium‐Triapine Analogues: In Cellulo MP FLIM and Zebrafish Live Imaging

Advanced Science, EarlyView.
Fluorescent BODIPY‐conjugated thiosemicarbazone ligands and their Ga(III), In(III), and Fe(III) complexes, inspired by Triapine, are developed as theranostic agents. Multiphoton FLIM and confocal microscopy in cancer cells and zebrafish reveal real‐time uptake, mitochondrial localisation, and whilst spectroscopic assays indicated preserved complex ...
Megan J. Green, Michael W. Jones, Merissa Saleem, Haobo Ge, Melita Tvardauskaite, Julia Dudzic, Fernando Cortezon‐Tamarit, Rory L. Arrowsmith, Charareh Pourzand, Gabriele Kociock‐Kohn, Nicholas H. Rees, Jonathan R. Dilworth, Stephen Faulkner, Stanley W. Botchway, David Gurevich, Sofia I. Pascu   +15 more
wiley   +1 more source

TME/NIR Dual‐Responsive Zinc‐Based Targeted Nanoagonist for Multimodal Amplification of STING‐Mediated Cancer Immunotherapy

Advanced Science, EarlyView.
A multifunctional nanoagonist (cDZ@IP) enables nano‐metabolite–driven multimodal activation of the STING pathway and enhanced immune recognition, achieving potent antitumor immunity and suppressing tumor growth and metastasis. This strategy highlights the rational design of therapeutic metabolites and establishes a new paradigm bridging nanomedicine ...
Kepeng Hu, Jiawei Wang, Wei Zhang, Zhixuan Wu, Jing Chen, Yujing He, Xiyue Duan, Yaoting He, Xin Xin, Haoyi Xiang, Yijing Wang, Chengwei Wu, Yang Yi, Qing Meng, Yuqian Qiao, Kui Cheng, Xiaojun Long, Zhangfa Song   +17 more
wiley   +1 more source

Metnase mediates resistance to topoisomerase II inhibitors in breast cancer cells. [PDF]

PLoS ONE, 2009
DNA replication produces tangled, or catenated, chromatids, that must be decatenated prior to mitosis or catastrophic genomic damage will occur. Topoisomerase IIalpha (Topo IIalpha) is the primary decatenating enzyme.
Justin Wray, Elizabeth A Williamson, Melanie Royce, Montaser Shaheen, Brian D Beck, Suk-Hee Lee, Jac A Nickoloff, Robert Hromas   +7 more
doaj   +1 more source

FOS3D: A Fluorescence‐Enabled Toolkit for Characterizing a Three‐dimensional Osteosarcoma Model

Advanced Science, EarlyView.
FOS3D describes fluorescent (F) osteosarcoma (OS) cells in a tri‐dimensional (3D) model. The study comprises three phases: development, where biofabrication parameters are tuned to achieve cytocompatibility and tumor‐specific mechanical properties in cell‐laden gelatin methacryloyl constructs; validation, where whole‐well fluorescence reading is ...
William Humble, Wiktor Zywicki, Enrico Lucarelli, Ania Naila Guerrieri, Francesca Taraballi, Gianluca Cidonio, Claudia Di Bella, Carmine Onofrillo, Andrea J. O'Connor, Serena Duchi   +9 more
wiley   +1 more source

RECENT ADVANCES ON NEW QUINAZOLINE DERIVATIVES AS DNA INTERCALATORS AND TOPOISOMERASE II INHIBITORS [PDF]

Al-Azhar Journal of Pharmaceutical Sciences
يُعدّ السرطان عبئًا صحيًا عالميًا كبيرًا، ينشأ عن النمو غير المنضبط للخلايا غير الطبيعية التي تُعيق وظائف الجسم الطبيعية. ويركّز جزء كبير من علاج السرطان على المركبات التي تستهدف الحمض النووي أو الإنزيمات المرتبطة به، مما يُعطّل العمليات الخلوية الأساسية
Hazem Mahdy, Amr Helmy, Mamdouh Mohamed
doaj   +1 more source

Prostaglandins Isolated from the Octocoral Plexaura homomalla: In Silico and In Vitro Studies Against Different Enzymes of Cancer

Marine Drugs, 2020
Prostaglandin A2-AcMe (1) and Prostaglandin A2 (2) were isolated from the octocoral Plexaura homomalla and three semisynthetic derivatives (3−5) were then obtained using a reduction protocol.
Diana Ximena Hurtado, Fabio A. Castellanos, Ericsson Coy-Barrera, Edisson Tello   +3 more
doaj   +1 more source

Conformational Snapshots of CydDC in a Native Lipid Bilayer Coupling Heme Transport to Antibiotic Resistance

Advanced Science, EarlyView.
Phylogenetic and biochemical analyses of the heme transporter CydDC reveal its functional conservation throughout bacterial evolution and demonstrate its unique asymmetric allosteric mechanism. Furthermore, impairment of CydDC function directly affects bacterial antibiotic resistance and likely compromises antibiotic efficacy through drug efflux.
Lili Yang, Changbin Zhang, Mengyuan Lyu, Yongbo Luo, Jierou Zhang, Yujiao Chen, Lintao Luo, Wen Qiao, Xiangyangpeng Li, Yu Zhou, Zhongling Wei, Yuling Xiao, Qian Niu, Juan Zhou, Guanglin He, Binwu Ying, Zhaoming Su, Hao Chen, Xiaodi Tang, Haohao Dong   +19 more
wiley   +1 more source