Results 41 to 50 of about 5,837 (209)

Novel Lysosome-Targeting Fluorescence Off-On Photosensitizer for Near-Infrared Hypoxia Imaging and Photodynamic Therapy In Vitro and In Vivo

open access: yesMolecules, 2022
Photodynamic therapy (PDT) has emerged as a new antitumor modality. Hypoxia, a vital characteristic of solid tumors, can be explored to stimulate the fluorescence response of photosensitizers (PSs).
Shangli Ding   +6 more
doaj   +1 more source

Intracellular complexities of acquiring a new enzymatic function revealed by mass-randomisation of active-site residues

open access: yeseLife, 2020
Selection for a promiscuous enzyme activity provides substantial opportunity for competition between endogenous and newly-encountered substrates to influence the evolutionary trajectory, an aspect that is often overlooked in laboratory directed evolution
Kelsi R Hall   +10 more
doaj   +1 more source

CYP1A1 and Cnr nitroreductase bioactivated niclosamide in vitro [PDF]

open access: yesMutagenesis, 2013
Abstract Niclosamide produces genotoxic effects, such as point mutations in Salmonella sp., sperm-head abnormalities in mice and clastogenic effects in human lymphocytes in vitro and in vivo. As cytochrome P450 could be involved in the bioactivation of niclosamide, we investigated which subfamily was involved.
Evelyn, Beristain-Castillo   +3 more
openaire   +2 more sources

Hypoxia-Inducible Regulation of a Prodrug-Activating Enzyme for Tumor-Specific Gene Therapy

open access: yesNeoplasia: An International Journal for Oncology Research, 2002
Previous studies have suggested that tumor hypoxia could be exploited for cancer gene therapy. Using hypoxia-responsive elements derived from the human vascular endothelial growth factor gene, we have generated vectors expressing a bacterial ...
Toru Shibata   +2 more
doaj   +1 more source

Engineering an asymmetric rhodamine dye suitable for developing ratiometric fluorescent probe

open access: yesSmart Molecules, 2023
Fluorescent probes based on rhodamine skeleton are extensively used in biological imaging. However, the construction of ratiometric fluorescent probes based on the rhodamine skeleton without introducing additional fluorophores is still challenging ...
Feiyu Yang   +4 more
doaj   +1 more source

Nitroreductase-Mediated Release of Inhibitors of Lysine-Specific Demethylase 1 (LSD1) from Prodrugs in Transfected Acute Myeloid Leukaemia Cells

open access: yes, 2019
Lysine-specific demethylase 1 (LSD1) has evolved as a promising therapeutic target for cancer treatment, especially in acute myeloid leukaemia (AML). To approach the challenge of site-specific LSD1 inhibition, we developed an enzyme-prodrug system with ...
Simon Steimle (7525388)   +10 more
core   +1 more source

Megazol and its bioisostere 4H-1,2,4-triazole: comparing the trypanocidal, cytotoxic and genotoxic activities and their in vitro and in silico interactions with the Trypanosoma brucei nitroreductase enzyme

open access: yesMemorias do Instituto Oswaldo Cruz, 2014
Megazol (7) is a 5-nitroimidazole that is highly active against Trypanosoma cruzi and Trypanosoma brucei, as well as drug-resistant forms of trypanosomiasis.
Alcione Silva de Carvalho   +8 more
doaj   +1 more source

Nitroreductase-Activatable Theranostic Molecules with High PDT Efficiency under Mild Hypoxia Based on a TADF Fluorescein Derivative

open access: yes, 2019
High specificity detection and site-specific therapy are still the main challenges for theranostic anticancer prodrugs. In this work, we reported two smart activatable theranostic molecules based on a thermally activated delayed fluorescence fluorescein ...
Gagik Gurzadyan   +15 more
core   +1 more source

Strategies of Detecting Bacteria Using Fluorescence-Based Dyes

open access: yesFrontiers in Chemistry, 2021
Identification of bacterial strains is critical for the theranostics of bacterial infections and the development of antibiotics. Many organic fluorescent probes have been developed to overcome the limitations of conventional detection methods.
Shin A Yoon   +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

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