Mode of action of the chloroethylating and carbamoylating moieties of the prodrug cloretazine.

Mode of action of the chloroethylating and carbamoylating moieties of the prodrug cloretazine.

Item
http://www.wikidata.org/entity/Q37187176
Reductive activation of the prodrug 1,2-bis(methylsulfonyl)-1-(2-chloroethyl)-2-[[1-(4-nitrophenyl)ethoxy]carbonyl]hydrazine (KS119) selectively occurs in oxygen-deficient cells and overcomes O(6)-alkylguanine-DNA alkyltransferase mediated KS119 tumLethality to leukemia cell lines of DNA interstrand cross-links generated by Cloretazine derived alkylating species.Inhibition of human DNA polymerase beta activity by the anticancer prodrug Cloretazine.Distinct mechanisms of cell-kill by triapine and its terminally dimethylated derivative Dp44mT due to a loss or gain of activity of their copper(II) complexes.Quantitative relationship between guanine O(6)-alkyl lesions produced by Onrigin™ and tumor resistance by O(6)-alkylguanine-DNA alkyltransferase.KS900: A hypoxia-directed, reductively activated methylating antitumor prodrug that selectively ablates O(6)-alkylguanine-DNA alkyltransferase in neoplastic cells.4-nitrobenzyloxycarbonyl derivatives of O(6)-benzylguanine as hypoxia-activated prodrug inhibitors of O(6)-alkylguanine-DNA alkyltransferase (AGT), which produces resistance to agents targeting the O-6 position of DNA guanine.A strategy for selective O(6)-alkylguanine-DNA alkyltransferase depletion under hypoxic conditions.Thioredoxin reductase is inhibited by the carbamoylating activity of the anticancer sulfonylhydrazine drug laromustine.Preclinical evaluation of Laromustine for use in combination with radiation therapy in the treatment of solid tumorsTumor-associated mutations in O⁶ -methylguanine DNA-methyltransferase (MGMT) reduce DNA repair functionality.Laromustine (cloretazine).Quantification of DNA interstrand crosslinks induced by ACNU in NIH/3T3 and L1210 cells using high-performance liquid chromatography/electrospray ionization tandem mass spectrometry.tert-Butyl N-[N,N-bis-(2-chloro-ethyl)sulfamo-yl]-N-(2-chloro-ethyl)carbamate.Clinical activity of laromustine (Onrigin™) in hematologic malignancies.pH-dependent general base catalyzed activation rather than isocyanate liberation may explain the superior anticancer efficacy of laromustine compared to related 1,2-bis(methylsulfonyl)-1-(2-chloroethyl)hydrazine prodrugs.
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Mode of action of the chloroethylating and carbamoylating moieties of the prodrug cloretazine.

Item
http://www.wikidata.org/entity/Q37187176
description
article científic
@ca
article scientifique
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articolo scientifico
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artigo científico
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bilimsel makale
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scientific article published on April 2006
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vedecký článok
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vetenskaplig artikel
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videnskabelig artikel
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vědecký článek
@cs
name
Mode of action of the chloroet ...... es of the prodrug cloretazine.
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Mode of action of the chloroet ...... es of the prodrug cloretazine.
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label
Mode of action of the chloroet ...... es of the prodrug cloretazine.
@en
Mode of action of the chloroet ...... es of the prodrug cloretazine.
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prefLabel
Mode of action of the chloroet ...... es of the prodrug cloretazine.
@en
Mode of action of the chloroet ...... es of the prodrug cloretazine.
@nl
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Mode of action of the chloroet ...... es of the prodrug cloretazine.
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10.1158/1535-7163.MCT-05-0532
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