Results 91 to 100 of about 239,934 (269)

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

Pharmacokinetics [PDF]

QJM, 1996
openaire   +2 more sources

Inhibition of SIRT7 Overcomes Radioresistance in Pancreatic Neuroendocrine Tumors by Reactivating MEN1 Expression

Advanced Science, EarlyView.
Pancreatic neuroendocrine tumors frequently silence MEN1 through epigenetic mechanisms. Here, SIRT7 recruits DNMT1 to the MEN1 promoter, drives hypermethylation, and enhances DNA repair. Inhibiting SIRT7 restores MEN1, reduces MRN complex abundance, impairs double‐strand break repair, and sensitizes PanNET models to radiation, supporting SIRT7 as a ...
Jianyun Jiang, Yan Wang, Yi Qin, Luohai Chen, Xiaowu Xu, Guixiong Fan, Desheng Jing, Miaoyan Wei, Xianjun Yu, Junfeng Xu, Shunrong Ji, Jie Chen   +11 more
wiley   +1 more source

Covalent Inhibition of SHMT2 by Gambogic Acid Induces Ferroptosis Through Mitochondrial Collapse in Triple‐Negative Breast Cancer

Advanced Science, EarlyView.
In this study, chemoproteomics combined with genetic and functional analyses was integrated to identify SHMT2 as a covalent and functional target of gambogic acid (GA) in triple‐negative breast cancer (TNBC). Further validation demonstrated that GA selectively modifies the Cys241 site of SHMT2, triggering mitochondrial dysfunction, activating the Nrf2 ...
Tong Yang, Chong Qiu, Yulei Li, Ying Zhang, Chen Wang, Jie Zhou, Zheng Chu, Ang Ma, Ling Huang, Yin Kwan Wong, Junzhe Zhang, Peng Gao, Cui Liu, Junhua Zhang, Huan Tang, Jigang Wang   +15 more
wiley   +1 more source

Machine learning to predict food effects during drug development: a comprehensive review

Journal of Cheminformatics
Drug absorption can be altered due to the consumption of food, impacting the efficacy and safety of the drug administered, and predicting food effects (FE) can be quite complex.
Alam Shah, Fulin Bi, Jin Yang
doaj   +1 more source

Quantitative Mass Spectrometry‐Based Biodistribution of Monoclonal Antibodies: An Alternative to Radio‐Biodistribution

Advanced Science, EarlyView.
Monoclonal antibodies are powerful anticancer therapeutics targeting tumor‐associated antigens. Mass spectrometry enables precise and accurate quantification of mAbs in tumor plasma and healthy organs. Unlike ligand binding assay and radioactivity, mass spectrometry does not suffer from matrix effects and labelling artefacts while facilitating method ...
Domenico Ravazza, Sheila Dakhel Plaza, Samuele Cazzamalli, Andrea Ciamarone, Andrea Galbiati, Riccardo Stucchi, Frederik Peissert, Emanuele Puca, Dario Neri, Ettore Gilardoni   +9 more
wiley   +1 more source

Pharmacologic Modulation of ARID3A with Rimegepant Reactivates Type I Interferon Signaling and Sensitizes Triple‐Negative Breast Cancer to PD‐1 Blockade

Advanced Science, EarlyView.
This study identifies ARID3A as a key immunosuppressive transcription factor in TNBC. Its inhibition activates the type I IFN pathway, boosting CD8+ T cell infiltration and sensitizing tumors to anti‐PD‐1. The FDA‐approved migraine drug Rimegepant targets ARID3A, enhances immunotherapy efficacy in preclinical models, and establishes a druggable axis to
Teng Zhou, Yifei Zhu, Cheng Zeng, Jinlu Han, Huiying Huang, Doudou Li, Mingxi Lin, Yizi Jin, Qin Guo, Yuxin Yan, Xinhui Mao, Yifei Zhou, Jian Zhang   +12 more
wiley   +1 more source

Carboranyl‐Curcuminoids for the Neutron Capture‐Based Treatment of Amyloid Aggregates in Alzheimer's Disease

Advanced Science, EarlyView.
The 10B‐enriched monocarbonyl analog of curcumin (BMAC) 10B‐9 enables site‐specific Boron Neutron Capture Therapy (BNCT) on amyloid‐β (Aβ) fibrils. Neutron irradiation induces histidine oxidation and fibril destabilization, as revealed by 1H‐NMR and FESEM analyses.
Sebastiano Micocci, Stefano Parisotto, Diego Alberti, Alberto Lanfranco, Valeria Bitonto, Polyssena Renzi, Martina Salmi, Andrea Magnani, Federica Dal Bello, Katiuscia Pagano, Laura Ragona, Nicoletta Protti, Annamaria Deagostino, Simonetta Geninatti Crich   +13 more
wiley   +1 more source

Active CNS delivery of oxycodone in healthy and endotoxemic pigs

Fluids and Barriers of the CNS
Background The primary objective of this study was to advance our understanding of active drug uptake at brain barriers in higher species than rodents, by examining oxycodone brain concentrations in pigs.
Frida Bällgren, Tilda Bergfast, Aghavni Ginosyan, Jessica Mahajan, Miklós Lipcsey, Margareta Hammarlund-Udenaes, Stina Syvänen, Irena Loryan   +7 more
doaj   +1 more source

Stress History Establishes a Transient Tolerant State That Shapes Antibiotic Survival Upon Resuscitation

Advanced Science, EarlyView.
High‐throughput single‐cell analysis of resuscitating bacteria reveals a starvation‐history‐dependent transiently tolerant subpopulation that survives β$\beta$‐lactam exposure by temporarily reducing growth. Distinct from classical persisters, these actively growing yet dynamically modulated cells dominate survival across clinically relevant antibiotic
Kieran Abbott, Georgeos Hardo, Ruizhe Li, Jack Bradley, Ashraf Zarkan, Somenath Bakshi   +5 more
wiley   +1 more source