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 |
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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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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. 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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.</description><subject>Animals</subject><subject>Antigens, Neoplasm</subject><subject>Antineoplastic Agents - pharmacology</subject><subject>Cell Line</subject><subject>DNA - metabolism</subject><subject>DNA Topoisomerases, Type II</subject><subject>DNA-Binding Proteins</subject><subject>Dose-Response Relationship, Drug</subject><subject>Enzyme Inhibitors - pharmacology</subject><subject>Guanidine - pharmacology</subject><subject>Isoenzymes - antagonists & inhibitors</subject><subject>Kidney - cytology</subject><subject>Kidney - drug effects</subject><subject>Kidney - enzymology</subject><subject>Protein Denaturation</subject><subject>Quinoxalines - pharmacology</subject><subject>Sulfanilamides - pharmacology</subject><subject>Topoisomerase II Inhibitors</subject><issn>0008-5472</issn><fulltext>true</fulltext><rsrctype>article</rsrctype><creationdate>2000</creationdate><recordtype>article</recordtype><sourceid>EIF</sourceid><recordid>eNo1j0tLxDAUhbNQnHH0L0iWuijepkmTLKX4KAyKOPvhprllIm1Tmynov7f4WB0OH3ycc8LWAGAyJbVYsfOU3peqclBnbJXnYJQCvWav1aGLU_yYwxA_sQsD8TR3bRywD5749fNbxYvCAsgbHhJHfoxjDCn2NGEiXtfYjQe8dXRE_gOGC3baYpfo8i83bPdwv6uesu3LY13dbbNxWZQhqcYSlG2urHAl5Qad1K5cGFmBngRA64WWxpQlKFFowMY1XrTWSq10sWFXv9pxdj35_TiFHqev_f-14huicUgy</recordid><startdate>20001101</startdate><enddate>20001101</enddate><creator>Gao, H</creator><creator>Yamasaki, E F</creator><creator>Chan, K K</creator><creator>Shen, L L</creator><creator>Snapka, R M</creator><scope>CGR</scope><scope>CUY</scope><scope>CVF</scope><scope>ECM</scope><scope>EIF</scope><scope>NPM</scope></search><sort><creationdate>20001101</creationdate><title>Chloroquinoxaline sulfonamide (NSC 339004) is a topoisomerase IIalpha/beta poison</title><author>Gao, H ; Yamasaki, E F ; Chan, K K ; Shen, L L ; Snapka, R M</author></sort><facets><frbrtype>5</frbrtype><frbrgroupid>cdi_FETCH-LOGICAL-p547-ae5c9e06f1592b6e18ab47b6547e92ade200fd2748866052370acbcd2f9947573</frbrgroupid><rsrctype>articles</rsrctype><prefilter>articles</prefilter><language>eng</language><creationdate>2000</creationdate><topic>Animals</topic><topic>Antigens, Neoplasm</topic><topic>Antineoplastic Agents - pharmacology</topic><topic>Cell Line</topic><topic>DNA - metabolism</topic><topic>DNA Topoisomerases, Type II</topic><topic>DNA-Binding Proteins</topic><topic>Dose-Response Relationship, Drug</topic><topic>Enzyme Inhibitors - pharmacology</topic><topic>Guanidine - pharmacology</topic><topic>Isoenzymes - antagonists & inhibitors</topic><topic>Kidney - cytology</topic><topic>Kidney - drug effects</topic><topic>Kidney - enzymology</topic><topic>Protein Denaturation</topic><topic>Quinoxalines - pharmacology</topic><topic>Sulfanilamides - pharmacology</topic><topic>Topoisomerase II Inhibitors</topic><toplevel>peer_reviewed</toplevel><toplevel>online_resources</toplevel><creatorcontrib>Gao, H</creatorcontrib><creatorcontrib>Yamasaki, E F</creatorcontrib><creatorcontrib>Chan, K K</creatorcontrib><creatorcontrib>Shen, L L</creatorcontrib><creatorcontrib>Snapka, R M</creatorcontrib><collection>Medline</collection><collection>MEDLINE</collection><collection>MEDLINE (Ovid)</collection><collection>MEDLINE</collection><collection>MEDLINE</collection><collection>PubMed</collection><jtitle>Cancer research (Chicago, Ill.)</jtitle></facets><delivery><delcategory>Remote Search Resource</delcategory><fulltext>fulltext</fulltext></delivery><addata><au>Gao, H</au><au>Yamasaki, E F</au><au>Chan, K K</au><au>Shen, L L</au><au>Snapka, R M</au><format>journal</format><genre>article</genre><ristype>JOUR</ristype><atitle>Chloroquinoxaline sulfonamide (NSC 339004) is a topoisomerase IIalpha/beta poison</atitle><jtitle>Cancer research (Chicago, Ill.)</jtitle><addtitle>Cancer Res</addtitle><date>2000-11-01</date><risdate>2000</risdate><volume>60</volume><issue>21</issue><spage>5937</spage><pages>5937-</pages><issn>0008-5472</issn><abstract>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.</abstract><cop>United States</cop><pmid>11085507</pmid></addata></record> |
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source | MEDLINE; American Association for Cancer Research; EZB-FREE-00999 freely available EZB journals |
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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