Targeting DNA topoisomerase IIα (TOP2A) in the hypoxic tumour microenvironment using unidirectional hypoxia‐activated prodrugs (uHAPs)
Sign Up to like & getrecommendations! Published in 2022 at "Iubmb Life"
DOI: 10.1002/iub.2619
Abstract: The hypoxic tumour microenvironment (hTME), arising from inadequate and chaotic vascularity, can present a major obstacle for the treatment of solid tumours. Hypoxic tumour cells compromise responses to treatment since they can generate resistance to… read more here.
Keywords: tumour microenvironment; unidirectional hypoxia; top2a; activated prodrugs ... See more keywords
Hypoxia Activated Fluorescent Probe Based on Self-immolative Block Copolymer.
Sign Up to like & getrecommendations! Published in 2022 at "Macromolecular bioscience"
DOI: 10.1002/mabi.202100417
Abstract: This work reported a hypoxia activated fluorescent probe for tumor imaging by using self-immolative block copolymer with azobenzene linkage. The water-soluble polymer composed of self-immolative building blocks showed no obvious fluorescence. Under the hypoxic microenvironment… read more here.
Keywords: activated fluorescent; block copolymer; immolative block; fluorescent probe ... See more keywords
Bioorthogonal chemistry and illumination controlled programmed size-changeable nanomedicine for synergistic photodynamic and hypoxia-activated therapy.
Sign Up to like & getrecommendations! Published in 2022 at "Biomaterials"
DOI: 10.1016/j.biomaterials.2022.121480
Abstract: Photodynamic therapy (PDT) can aggravate the hypoxia aggravation and be further utilized for the activation of hypoxia-activated prodrug (HAP). Ideally, photosensitizers (PSs) are mainly administrated to tumor vasculatures adjacent to regions with high oxygen to… read more here.
Keywords: hypoxia; hypoxia activated; hap; tumor ... See more keywords
Hypoxia-activated pro-drugs of the KDAC inhibitor vorinostat (SAHA)
Sign Up to like & getrecommendations! Published in 2020 at "Tetrahedron"
DOI: 10.1016/j.tet.2020.131170
Abstract: Abstract Hypoxia (lower than normal oxygen) is a characteristic of most solid tumours that results in poor cancer patient prognosis. The difference in cellular environment between normoxia (21% oxygen) or physoxia (4–7.5% oxygen) and hypoxia… read more here.
Keywords: hypoxia; pro drugs; kdac inhibitor; hypoxia activated ... See more keywords
Noncovalent Theranostic Prodrug for Hypoxia-Activated Drug Delivery and Real-Time Tracking.
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DOI: 10.1021/acs.analchem.1c03153
Abstract: Real-time tracking of hypoxia-activated prodrugs (HAPs) delivery and the release process is of great significance for innovative medical treatments and drug development. Existing theranostic methods for HAPs activation imaging are based on the covalent approach,… read more here.
Keywords: drug; drug delivery; hypoxia activated; theranostic prodrug ... See more keywords
Hypoxia-Activated Prodrug Enabling Synchronous Chemotherapy and HIF-1α Downregulation for Tumor Treatment.
Sign Up to like & getrecommendations! Published in 2021 at "Bioconjugate chemistry"
DOI: 10.1021/acs.bioconjchem.1c00131
Abstract: The overexpression of HIF-1α in solid tumors due to hypoxia is closely related to drug resistance and consequent treatment failure. Herein, we constructed a hypoxia-activated prodrug named as YC-Dox. This prodrug could be activated under… read more here.
Keywords: hif; tumor treatment; hif downregulation; hypoxia activated ... See more keywords
In Vivo Identification of Adducts from the New Hypoxia-Activated Prodrug CP-506 Using DNA Adductomics.
Sign Up to like & getrecommendations! Published in 2022 at "Chemical research in toxicology"
DOI: 10.1021/acs.chemrestox.1c00329
Abstract: Many chemotherapeutic drugs exert their cytotoxicity through the formation of DNA modifications (adducts), which interfere with DNA replication, an overactive process in rapidly dividing cancer cells. Side effects from the therapy are common, however, because… read more here.
Keywords: dna; hypoxia activated; vivo identification; dna adducts ... See more keywords
Hypoxia-Activated PEGylated Paclitaxel Prodrug Nanoparticles for Potentiated Chemotherapy.
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DOI: 10.1021/acsnano.2c05341
Abstract: Developing controlled drug-release systems is imperative and valuable for increasing the therapeutic index. Herein, we synthesized hypoxia-responsive PEGylated (PEG = poly(ethylene glycol)) paclitaxel prodrugs by utilizing azobenzene (Azo) as a cleavable linker. The as-fabricated prodrugs… read more here.
Keywords: paclitaxel prodrug; activated pegylated; hypoxia; pap nps ... See more keywords
Theranostic Liposomes with Hypoxia-Activated Prodrug to Effectively Destruct Hypoxic Tumors Post-Photodynamic Therapy.
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DOI: 10.1021/acsnano.6b07525
Abstract: Photodynamic therapy (PDT), a noninvasive cancer therapeutic method triggered by light, would lead to severe tumor hypoxia after treatment. Utilizing a hypoxia-activated prodrug, AQ4N, which only shows toxicity to cancer cells under hypoxic environment, herein,… read more here.
Keywords: photodynamic therapy; hypoxia activated; pdt; activated prodrug ... See more keywords
Phase 2 trial of hypoxia activated evofosfamide (TH302) for treatment of recurrent bevacizumab-refractory glioblastoma
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DOI: 10.1038/s41598-021-81841-0
Abstract: Evofosfamide (Evo or TH302) is a hypoxia-activated prodrug which is reduced leading to the release of alkylating agent bromo-isophosphoramide mustard, which has shown safety and signals of efficacy in a prior phase 1 study in… read more here.
Keywords: hypoxia activated; phase; bevacizumab refractory; refractory glioblastoma ... See more keywords
Autocatalytic oncotherapy nanosystem with glucose depletion for the cascade amplification of hypoxia-activated chemotherapy and H2O2-dependent chemodynamic therapy.
Sign Up to like & getrecommendations! Published in 2022 at "Biomaterials science"
DOI: 10.1039/d1bm01944a
Abstract: Employing hypoxia-activated prodrugs is an appealing oncotherapy strategy, but limited by insufficient tumor hypoxia. Moreover, a standalone prodrug fails to treat tumors satisfactorily due to tumor complexity. Herein, a nanosystem (TPZ@FeMSN-GOX) was established for triple… read more here.
Keywords: hypoxia; therapy; tpz femsn; hypoxia activated ... See more keywords