Matches in SemOpenAlex for { <https://semopenalex.org/work/W2885246716> ?p ?o ?g. }
Showing items 1 to 75 of
75
with 100 items per page.
- W2885246716 abstract "Hypoxia-selective antitumor prodrugs utilize the unique feature of most tumors -- hypoxia (low oxygen concentration), for therapeutic purpose and are widely studied in preclinical and clinical stages. Tirapazamine (TPZ, 3-amino-1,2,4-benzotriazine-1,4-di-N-oxide) is a hypoxiaselective cytotoxin that has been examined in Phase II and III clinical trials. The mechanism of DNA strand cleavage by TPZ and its analogs is still unknown. We described two isotopic labeling studies followed by MS analysis to explain the DNA strand cleavage of TPZs. One is to use desamino TPZ (1,2,4-benzotriazine 1,4-di-Noxide) to provided evidence against the generation of benzotriazinyl radical intermediates. The other one is to use 18O-labeled TPZ and DMSO-diazonium salt derivatization to provide direct evidence for the generation of hydroxyl radical. At least two conditions are required for successful clinical application of hypoxiaselective prodrugs: i. target tumors must be hypoxic and ii. appropriate enzymes involved in bioactivation of the drug must be expressed in the tissue. In this regard, it will be necessary to develop diagnostic probes to assess the expression of these enzymes. Here we described tirapazamine analogs as pro-fluorescent substrates of enzymes that catalyze the bioreductive activation of hypoxia-selective prodrugs. That is, the reduced metabolites generated by one-electron enzymatic activation of these compounds under hypoxic condition are fluorescent, while the parent compounds are non-fluorescent. Our results could facilitate the development of useful fluorescent probes in detecting one electron reductases involved in bioactivation of hypoxia-selective antitumor prodrugs." @default.
- W2885246716 created "2018-08-22" @default.
- W2885246716 creator A5082453888 @default.
- W2885246716 date "2021-04-14" @default.
- W2885246716 modified "2023-09-25" @default.
- W2885246716 title "Hypoxia-selective antitumor prodrugs and fluorescent probes" @default.
- W2885246716 doi "https://doi.org/10.32469/10355/62495" @default.
- W2885246716 hasPublicationYear "2021" @default.
- W2885246716 type Work @default.
- W2885246716 sameAs 2885246716 @default.
- W2885246716 citedByCount "0" @default.
- W2885246716 crossrefType "dissertation" @default.
- W2885246716 hasAuthorship W2885246716A5082453888 @default.
- W2885246716 hasBestOaLocation W28852467161 @default.
- W2885246716 hasConcept C108215921 @default.
- W2885246716 hasConcept C109316439 @default.
- W2885246716 hasConcept C121332964 @default.
- W2885246716 hasConcept C126322002 @default.
- W2885246716 hasConcept C178790620 @default.
- W2885246716 hasConcept C181199279 @default.
- W2885246716 hasConcept C185592680 @default.
- W2885246716 hasConcept C202751555 @default.
- W2885246716 hasConcept C21951064 @default.
- W2885246716 hasConcept C2776313096 @default.
- W2885246716 hasConcept C2779081379 @default.
- W2885246716 hasConcept C2781326480 @default.
- W2885246716 hasConcept C509974204 @default.
- W2885246716 hasConcept C540031477 @default.
- W2885246716 hasConcept C552990157 @default.
- W2885246716 hasConcept C55493867 @default.
- W2885246716 hasConcept C62520636 @default.
- W2885246716 hasConcept C71924100 @default.
- W2885246716 hasConcept C7836513 @default.
- W2885246716 hasConcept C86803240 @default.
- W2885246716 hasConcept C91881484 @default.
- W2885246716 hasConcept C98274493 @default.
- W2885246716 hasConceptScore W2885246716C108215921 @default.
- W2885246716 hasConceptScore W2885246716C109316439 @default.
- W2885246716 hasConceptScore W2885246716C121332964 @default.
- W2885246716 hasConceptScore W2885246716C126322002 @default.
- W2885246716 hasConceptScore W2885246716C178790620 @default.
- W2885246716 hasConceptScore W2885246716C181199279 @default.
- W2885246716 hasConceptScore W2885246716C185592680 @default.
- W2885246716 hasConceptScore W2885246716C202751555 @default.
- W2885246716 hasConceptScore W2885246716C21951064 @default.
- W2885246716 hasConceptScore W2885246716C2776313096 @default.
- W2885246716 hasConceptScore W2885246716C2779081379 @default.
- W2885246716 hasConceptScore W2885246716C2781326480 @default.
- W2885246716 hasConceptScore W2885246716C509974204 @default.
- W2885246716 hasConceptScore W2885246716C540031477 @default.
- W2885246716 hasConceptScore W2885246716C552990157 @default.
- W2885246716 hasConceptScore W2885246716C55493867 @default.
- W2885246716 hasConceptScore W2885246716C62520636 @default.
- W2885246716 hasConceptScore W2885246716C71924100 @default.
- W2885246716 hasConceptScore W2885246716C7836513 @default.
- W2885246716 hasConceptScore W2885246716C86803240 @default.
- W2885246716 hasConceptScore W2885246716C91881484 @default.
- W2885246716 hasConceptScore W2885246716C98274493 @default.
- W2885246716 hasLocation W28852467161 @default.
- W2885246716 hasOpenAccess W2885246716 @default.
- W2885246716 hasPrimaryLocation W28852467161 @default.
- W2885246716 hasRelatedWork W11011638 @default.
- W2885246716 hasRelatedWork W13550157 @default.
- W2885246716 hasRelatedWork W16268762 @default.
- W2885246716 hasRelatedWork W29124308 @default.
- W2885246716 hasRelatedWork W29328981 @default.
- W2885246716 hasRelatedWork W32098337 @default.
- W2885246716 hasRelatedWork W3211555 @default.
- W2885246716 hasRelatedWork W33499809 @default.
- W2885246716 hasRelatedWork W36047135 @default.
- W2885246716 hasRelatedWork W4704116 @default.
- W2885246716 isParatext "false" @default.
- W2885246716 isRetracted "false" @default.
- W2885246716 magId "2885246716" @default.
- W2885246716 workType "dissertation" @default.