Minor groove dimeric bisbenzimidazoles inhibit in vitro DNA binding to eukaryotic DNA topoisomerase I
The potential of six dimeric bisbenzimidazoles bound to scDNA to inhibit eukaryotic DNA topoisomerase (topo-I) was studied chemically; the tested compounds differed in linker structure and length. All the compounds inhibited topo-I, DB(7) being the most efficient; its inhibitory activity in vitro wa...
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| Veröffentlicht in: | Biochemistry (Moscow) 2010-06, Vol.75 (6), p.695-701 |
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| container_title | Biochemistry (Moscow) |
| container_volume | 75 |
| creator | Susova, O. Yu Ivanov, A. A. Morales Ruiz, S. S. Lesovaya, E. A. Gromyko, A. V. Streltsov, S. A. Zhuze, A. L. |
| description | The potential of six dimeric bisbenzimidazoles bound to scDNA to inhibit eukaryotic DNA topoisomerase (topo-I) was studied chemically; the tested compounds differed in linker structure and length. All the compounds inhibited topo-I, DB(7) being the most efficient; its inhibitory activity
in vitro
was 50-fold higher than that of camptothecin. It is noteworthy that inhibitory properties of nearly all the tested compounds increased many times if they were preincubated with scDNA for three days. |
| doi_str_mv | 10.1134/S0006297910060039 |
| format | Article |
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in vitro
was 50-fold higher than that of camptothecin. It is noteworthy that inhibitory properties of nearly all the tested compounds increased many times if they were preincubated with scDNA for three days.</description><identifier>ISSN: 0006-2979</identifier><identifier>EISSN: 1608-3040</identifier><identifier>DOI: 10.1134/S0006297910060039</identifier><identifier>PMID: 20636260</identifier><language>eng</language><publisher>Dordrecht: SP MAIK Nauka/Interperiodica</publisher><subject>Binding sites ; Biochemistry ; Biomedical and Life Sciences ; Biomedicine ; Bioorganic Chemistry ; Bisbenzimidazole - chemistry ; Bisbenzimidazole - pharmacology ; Chemical compounds ; Chemical properties ; Deoxyribonucleic acid ; Dimerization ; DNA ; DNA - metabolism ; DNA topoisomerase I ; DNA Topoisomerases, Type I - metabolism ; DNA-ligand interactions ; Enzymes ; Genetic transcription ; Inhibitor drugs ; Life Sciences ; Microbiology ; Protein Binding ; Topoisomerase I Inhibitors</subject><ispartof>Biochemistry (Moscow), 2010-06, Vol.75 (6), p.695-701</ispartof><rights>Pleiades Publishing, Ltd. 2010</rights><rights>COPYRIGHT 2010 Springer</rights><lds50>peer_reviewed</lds50><woscitedreferencessubscribed>false</woscitedreferencessubscribed><citedby>FETCH-LOGICAL-c469t-b354c6d27d06ed21e8dcd83cf75ae7d6563a00fbc665f785edbb4add28fa415b3</citedby><cites>FETCH-LOGICAL-c469t-b354c6d27d06ed21e8dcd83cf75ae7d6563a00fbc665f785edbb4add28fa415b3</cites></display><links><openurl>$$Topenurl_article</openurl><openurlfulltext>$$Topenurlfull_article</openurlfulltext><thumbnail>$$Tsyndetics_thumb_exl</thumbnail><linktopdf>$$Uhttps://link.springer.com/content/pdf/10.1134/S0006297910060039$$EPDF$$P50$$Gspringer$$H</linktopdf><linktohtml>$$Uhttps://link.springer.com/10.1134/S0006297910060039$$EHTML$$P50$$Gspringer$$H</linktohtml><link.rule.ids>314,780,784,27923,27924,41487,42556,51318</link.rule.ids><backlink>$$Uhttps://www.ncbi.nlm.nih.gov/pubmed/20636260$$D View this record in MEDLINE/PubMed$$Hfree_for_read</backlink></links><search><creatorcontrib>Susova, O. Yu</creatorcontrib><creatorcontrib>Ivanov, A. A.</creatorcontrib><creatorcontrib>Morales Ruiz, S. S.</creatorcontrib><creatorcontrib>Lesovaya, E. A.</creatorcontrib><creatorcontrib>Gromyko, A. V.</creatorcontrib><creatorcontrib>Streltsov, S. A.</creatorcontrib><creatorcontrib>Zhuze, A. L.</creatorcontrib><title>Minor groove dimeric bisbenzimidazoles inhibit in vitro DNA binding to eukaryotic DNA topoisomerase I</title><title>Biochemistry (Moscow)</title><addtitle>Biochemistry Moscow</addtitle><addtitle>Biochemistry (Mosc)</addtitle><description>The potential of six dimeric bisbenzimidazoles bound to scDNA to inhibit eukaryotic DNA topoisomerase (topo-I) was studied chemically; the tested compounds differed in linker structure and length. All the compounds inhibited topo-I, DB(7) being the most efficient; its inhibitory activity
in vitro
was 50-fold higher than that of camptothecin. It is noteworthy that inhibitory properties of nearly all the tested compounds increased many times if they were preincubated with scDNA for three days.</description><subject>Binding sites</subject><subject>Biochemistry</subject><subject>Biomedical and Life Sciences</subject><subject>Biomedicine</subject><subject>Bioorganic Chemistry</subject><subject>Bisbenzimidazole - chemistry</subject><subject>Bisbenzimidazole - pharmacology</subject><subject>Chemical compounds</subject><subject>Chemical properties</subject><subject>Deoxyribonucleic acid</subject><subject>Dimerization</subject><subject>DNA</subject><subject>DNA - metabolism</subject><subject>DNA topoisomerase I</subject><subject>DNA Topoisomerases, Type I - metabolism</subject><subject>DNA-ligand interactions</subject><subject>Enzymes</subject><subject>Genetic transcription</subject><subject>Inhibitor drugs</subject><subject>Life Sciences</subject><subject>Microbiology</subject><subject>Protein Binding</subject><subject>Topoisomerase I Inhibitors</subject><issn>0006-2979</issn><issn>1608-3040</issn><fulltext>true</fulltext><rsrctype>article</rsrctype><creationdate>2010</creationdate><recordtype>article</recordtype><sourceid>EIF</sourceid><sourceid>ABUWG</sourceid><sourceid>AFKRA</sourceid><sourceid>AZQEC</sourceid><sourceid>BENPR</sourceid><sourceid>CCPQU</sourceid><sourceid>DWQXO</sourceid><sourceid>GNUQQ</sourceid><recordid>eNqFkktv1DAUhS0EokPhB7BBFiy6SrmOH0mWo0KhUoEFsLYc-2ZwSezBTirRX4-jKSBeQl5c2ec7x762CXnM4JQxLp6_BwBVd03HSgXg3R2yYQraioOAu2SzytWqH5EHOV-VaQ0dv0-OalBc1Qo2BN_4EBPdpRivkTo_YfKW9j73GG785J25iSNm6sMn3_u5VHrt5xTpi7fbggXnw47OkeLy2aSvcS7mVZnjPvocS5rJSC8eknuDGTM-uq3H5OP5yw9nr6vLd68uzraXlRWqm6ueS2GVqxsHCl3NsHXWtdwOjTTYOCUVNwBDb5WSQ9NKdH0vjHN1OxjBZM-Pyckhd5_ilwXzrCefLY6jCRiXrBspJBdSif-TnHdtKyUU8ulv5FVcUihtaNm0ogUJTYGeHaCdGVH7MMQ5GbtG6m3ZUKiai65Qp3-hynA4eRsDDr6s_2JgB4NNMeeEg94nP5WL1gz0-gX0H1-geJ7cnnfpJ3Q_HN_fvAD1AchFCjtMPxv6d-o3V-G5aQ</recordid><startdate>20100601</startdate><enddate>20100601</enddate><creator>Susova, O. 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Yu ; Ivanov, A. A. ; Morales Ruiz, S. S. ; Lesovaya, E. A. ; Gromyko, A. V. ; Streltsov, S. A. ; Zhuze, A. 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| ispartof | Biochemistry (Moscow), 2010-06, Vol.75 (6), p.695-701 |
| issn | 0006-2979 1608-3040 |
| language | eng |
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| source | MEDLINE; SpringerLink Journals - AutoHoldings |
| subjects | Binding sites Biochemistry Biomedical and Life Sciences Biomedicine Bioorganic Chemistry Bisbenzimidazole - chemistry Bisbenzimidazole - pharmacology Chemical compounds Chemical properties Deoxyribonucleic acid Dimerization DNA DNA - metabolism DNA topoisomerase I DNA Topoisomerases, Type I - metabolism DNA-ligand interactions Enzymes Genetic transcription Inhibitor drugs Life Sciences Microbiology Protein Binding Topoisomerase I Inhibitors |
| title | Minor groove dimeric bisbenzimidazoles inhibit in vitro DNA binding to eukaryotic DNA topoisomerase I |
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