Results 51 to 60 of about 20,922 (255)

The effect of lengths of branched-chain fatty alcohols on the efficacy and safety of docetaxel-prodrug nanoassemblies

open access: yesActa Pharmaceutica Sinica B
The self-assembly prodrugs are usually consisted of drug modules, activation modules, and assembly modules. Keeping the balance between efficacy and safety by selecting suitable modules remains a challenge for developing prodrug nanoassemblies.
Shuo Wang   +10 more
doaj   +1 more source

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

open access: yesAdvanced 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   +15 more
wiley   +1 more source

N-Monosubstituted Methoxy-oligo(ethylene glycol) Carbamate Ester Prodrugs of Resveratrol

open access: yesMolecules, 2015
Resveratrol is a natural polyphenol with many interesting biological activities. Its pharmacological exploitation in vivo is, however, hindered by its rapid elimination via phase II conjugative metabolism at the intestinal and, most importantly, hepatic ...
Andrea Mattarei   +4 more
doaj   +1 more source

Engineering Prodrug Nanomedicine for Cancer Immunotherapy

open access: yesAdvanced Science, 2020
Immunotherapy has shifted the clinical paradigm of cancer management. However, despite promising initial progress, immunotherapeutic approaches to cancer still suffer from relatively low response rates and the possibility of severe side effects, likely ...
Bin Yang   +4 more
doaj   +1 more source

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

open access: yesAdvanced 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   +4 more
wiley   +1 more source

Unlocking a Nitrosuccinate Lyase for Decarboxylative Enzymatic Hydronitration

open access: yesAngewandte 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   +9 more
wiley   +2 more sources

Streptavidins Coordinate Biotin Sequestration and Self‐Resistance Within a Biotin‐Pathway Antibiotic Network

open access: yesAdvanced Science, EarlyView.
A conserved genomic region between two streptavidin genes in Streptomyces packages biosynthetic gene clusters for diverse biotin‐pathway antibiotics: acidomycin, stravidin, the new non‐proteinogenic amino acid ANDA, and the new BioA inhibitor α‐methyl‐KAPA.
Sumire Kurosawa   +8 more
wiley   +1 more source

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

open access: yesAngewandte 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   +14 more
wiley   +2 more sources

Flurbiprofen–antioxidant mutual prodrugs as safer nonsteroidal anti-inflammatory drugs: synthesis, pharmacological investigation, and computational molecular modeling

open access: yesDrug Design, Development and Therapy, 2016
Zaman Ashraf,1,2 Alamgeer,3 Munazza Kanwal,1 Mubashir Hassan,2 Sahar Abdullah,3 Mamuna Waheed,3 Haseeb Ahsan,3 Song Ja Kim2 1Department of Chemistry, Allama Iqbal Open University, Islamabad, Pakistan; 2Department of Biological Sciences, College of ...
Ashraf Z   +7 more
doaj  

tBid‐Mediated Genetic Ablation of Connective Tissue Cells Reveals Their Key Regulatory Function During Limb Regeneration in Axolotls

open access: yesAdvanced Science, EarlyView.
We establish a tBid‐mediated cell ablation system in axolotls, achieve rapid and efficient ablation of multiple cell types, including muscle stem cell, spinal cord cell, and connective tissue (CT) cells. We investigate the role of CT using tBid‐mediated CT ablation and identify its essential role for limb development and regeneration.
Yan Hu   +11 more
wiley   +1 more source

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