Results 61 to 70 of about 65,300 (300)

Tumor penetrating Janus prodrug nanoassemblies for enhanced synergistic chemotherapy and photodynamic therapy of colon cancer

Materials & Design
Intelligent nanodrug delivery systems that respond to tumor microenvironment have been extensively utilized in cancer therapy research. However, the passive diffusion of prodrug nanoparticles is hindered due to the absence of capillaries and dense ...
Ying Hao, Tailuo Liu, Runhao Xu, Bo Li, Ka Li, Yuwen Chen   +5 more
doaj   +1 more source

Esterase-Sensitive Prodrugs of a Potent Bisubstrate Inhibitor of Nicotinamide N-Methyltransferase (NNMT) Display Cellular Activity

Biomolecules, 2021
A recently discovered bisubstrate inhibitor of Nicotinamide N-methyltransferase (NNMT) was found to be highly potent in biochemical assays with a single digit nanomolar IC50 value but lacking in cellular activity.
Matthijs J. van Haren, Yongzhi Gao, Ned Buijs, Roberto Campagna, Davide Sartini, Monica Emanuelli, Lukasz Mateuszuk, Agnieszka Kij, Stefan Chlopicki, Pol Escudé Martinez de Castilla, Raymond Schiffelers, Nathaniel I. Martin   +11 more
doaj   +1 more source

Dual‐Responsive Dynamic Covalent Bond‐Based Assembly of Lipid‐Nanozyme Systems via Multi‐Target Synergy and Efficient Target Enrichment for Ischemic Stroke Therapy

Advanced Science, EarlyView.
This system adopts a biomimetic phospholipid structure, covalently binding iNOS inhibitors, neuroprotective agent PCA and vitamin E derivatives through pH/ROS dual‐responsive bonds, and assembles them with Prussian blue nanozyme to form PBB@AHA. It can efficiently penetrate the blood‐brain barrier and simultaneously release multiple active components ...
Mengcheng Guo, Qingran Guan, Guanyu Qiao, Lixue Zhang, Man Liu, Zhen Li, Qingbiao Yang, Meili Shen, Linlin Liu, Yapeng Li   +9 more
wiley   +1 more source

Cationic N,N-Dimethylglycine Ester Prodrug of 2R-α-Tocotrienol Promotes Intestinal Absorption via Efficient Self-Micellization with Intrinsic Bile Acid Anion

Molecules, 2022
The intestinal absorption of hydrophobic compounds is severely influenced by their transportation rate through the unstirred water layer in the intestinal lumen.
Daisuke Watase, Shuichi Setoguchi, Nami Nagata-Akaho, Shotaro Goto, Hirofumi Yamakawa, Ayano Yamada, Mitsuhisa Koga, Yoshiharu Karube, Kazuhisa Matsunaga, Jiro Takata   +9 more
doaj   +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

Unlocking a Nitrosuccinate Lyase for Decarboxylative Enzymatic Hydronitration

Angewandte Chemie, EarlyView.
The nitrosuccinate lyase CreD catalyzes C–NO2 bond formation using nitrite in water and shows synthetic practicality with high turnover numbers up to 102,000. A combination of protein engineering and computational methods helped to reveal the mechanistic principles that underpin this unique enzymatic activity.
Matteo Aleotti, Hannah Dreisbach, Rémi Corlay, Clara Weber, Tamara Reiter, Wael Elaily, Bastian Daniel, Klaus Zangger, Pedro A. Sánchez‐Murcia, Mélanie Hall   +9 more
wiley   +2 more sources

A prodrug activated by H2O2 and mitochondrial hydroxide: an improvement of cancer cells versus neutrophils selectivity

, 2023
Many known chemotherapeutic anticancer agents exhibit neutropenia as a dose-limiting side effect. In this paper we suggest a prodrug concept solving this problem for camptothecin (HO-cpt). The prodrug is programmed according to Boolean “AND” logic.
Tina, Jost, Itziar, Cossío Cuartero, Sabrina, Gensberger-Reigl, Viktor, Reshetnikov, Marit, Wondrak, Rainer, Tietze, Andrés, Hidalgo, Marlies, Körber, Frank, Beierlein, Petra, Imhof, Monika, Pischetsrieder, Subrata, Dutta, Rostyslav, Bilyy, Adrian, Wünsche, Insa, Klemt, Maximilian, Böhm, Leoni, Kunz-Schughart, Andriy, Mokhir, Galyna, Bila   +18 more
core   +1 more source

Glomage: A Multimodal Platform for High‐Content Morphological and RNA Profiling of Glomeruli in Zebrafish and Mouse Models

Advanced Science, EarlyView.
Understanding how glomeruli, the kidney's filtration units, function in intact tissue remains challenging. Glomage enables rapid 3D imaging and quantitative analysis of entire glomeruli from zebrafish larvae and mice. This approach allows scalable cell quantification and detection of structural changes, advancing kidney disease research and ...
Maximilian Schindler, Tim Lange, Sophia‐Marie Bach, Soeren S. Lienkamp, Nicole Endlich   +4 more
wiley   +1 more source

Chemically Regulated STING‐Activating Prodrugs of Deoxyribose Cyclic Dinucleotides Elicit Robust Immune Activation and Durable Antitumor Immunity

Angewandte Chemie, EarlyView.
All three diastereoisomers of an esterase‐sensitive phosphotriester dCDN prodrug demonstrate improved activity. The (Rp,Rp) diastereoisomer shows the highest activity with an EC50 of 1.7 nM in STING activation and displays the most pronounced antitumor activity via intravenous administration, significantly suppressing tumor proliferation, extending the
Zhiqiang Xie, Huimin Liu, Yuchen Yang, Xiaohan Sun, Jingwen Wang, Tianxiang Liu, Baifan Wang, Wenrui Qiu, Yiwen Sun, Yuting Bai, Yao Zhang, Dejun Ma, Rong Xiang, Shibo Li, Zhen Xi   +14 more
wiley   +2 more sources

Eradication of Cancer Cells Using Doxifluridine and Mesenchymal Stem Cells Expressing Thymidine Phosphorylase

Bioengineering
Gene-directed enzyme prodrug therapy (GDEPT) has been developed over several decades as a targeted cancer treatment aimed at minimizing toxicity to healthy cells. This approach involves three key components: a non-toxic prodrug, a gene encoding an enzyme
Xutu Wang, Ian Peng, Ching-An Peng
doaj   +1 more source