Chloroquinoxaline sulfonamide (NSC 339004) is a topoisomerase IIalpha/beta poison

Chloroquinoxaline sulfonamide (chlorosulfaquinoxaline, CQS, NSC 339004) is active against murine and human solid tumors. On the basis of its structural similarity to the topoisomerase IIbeta-specific drug XK469, CQS was tested and found to be both a topoisomerase-IIalpha and a topoisomerase-IIbeta p...

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Veröffentlicht in:Cancer research (Chicago, Ill.) Ill.), 2000-11, Vol.60 (21), p.5937
Hauptverfasser: Gao, H, Yamasaki, E F, Chan, K K, Shen, L L, Snapka, R M
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creator Gao, H
Yamasaki, E F
Chan, K K
Shen, L L
Snapka, R M
description Chloroquinoxaline sulfonamide (chlorosulfaquinoxaline, CQS, NSC 339004) is active against murine and human solid tumors. On the basis of its structural similarity to the topoisomerase IIbeta-specific drug XK469, CQS was tested and found to be both a topoisomerase-IIalpha and a topoisomerase-IIbeta poison. Topoisomerase II poisoning by CQS is essentially undetectable in assays using the common protein denaturant SDS, but easily detectable with strong chaotropic protein denaturants. The finding that detection of topoisomerase poisoning can be so dependent on the protein denaturant used in the assay has implications for drug discovery efforts and for our understanding of topoisomerase poisons.
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subjects Animals
Antigens, Neoplasm
Antineoplastic Agents - pharmacology
Cell Line
DNA - metabolism
DNA Topoisomerases, Type II
DNA-Binding Proteins
Dose-Response Relationship, Drug
Enzyme Inhibitors - pharmacology
Guanidine - pharmacology
Isoenzymes - antagonists & inhibitors
Kidney - cytology
Kidney - drug effects
Kidney - enzymology
Protein Denaturation
Quinoxalines - pharmacology
Sulfanilamides - pharmacology
Topoisomerase II Inhibitors
title Chloroquinoxaline sulfonamide (NSC 339004) is a topoisomerase IIalpha/beta poison
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