Distamycin A and tallimustine inhibit TBP binding and basal in vitro transcription
The antibiotic distamycin A is a DNA minor groove binding drug (MGB) that recognizes a stretch of a least four ATs. The alkylating benzoyl mustard derivative tallimustine (FCE 24517) has powerfull anti-tumor activity. Using the electrophoretic mobility shift assay (EMSA) we determined that both comp...
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| Veröffentlicht in: | Nucleic acids research 1995-05, Vol.23 (10), p.1657-1663 |
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| creator | Bellorini, Marianna Moncollin, Vincent D'lncalci, Maurizio Mongelli, Nicola Mantovani, Roberto |
| description | The antibiotic distamycin A is a DNA minor groove binding drug (MGB) that recognizes a stretch of a least four ATs. The alkylating benzoyl mustard derivative tallimustine (FCE 24517) has powerfull anti-tumor activity. Using the electrophoretic mobility shift assay (EMSA) we determined that both compounds can prevent binding of TBP and, with 10-fold higher concentration, TBP-TFIIA (DA) and TBP-TRIA-TFIIB (DAB) to a TATA box. Once formed, the DA and DAB complexes are more resistant to MGB challenge. Both drugs can inhibit basal In vitro transcription of a minimal TATA-containlng promoter and similar concentrations are necessary for binding and transcrip-tional inhibition. Tallimustine shows strong selectivity by decreasing only correctly initiated transcripts. Even at high doses (20μM), however, they cannot disturb a competent pre-initiation complex or Pol II progression. This functional in vitro model will provide a way to investigate the activity of sequence-specific DNA binding drugs with potential anti-viral and anti-tumour activity and to develop novel more selective compounds. |
| doi_str_mv | 10.1093/nar/23.10.1657 |
| format | Article |
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The alkylating benzoyl mustard derivative tallimustine (FCE 24517) has powerfull anti-tumor activity. Using the electrophoretic mobility shift assay (EMSA) we determined that both compounds can prevent binding of TBP and, with 10-fold higher concentration, TBP-TFIIA (DA) and TBP-TRIA-TFIIB (DAB) to a TATA box. Once formed, the DA and DAB complexes are more resistant to MGB challenge. Both drugs can inhibit basal In vitro transcription of a minimal TATA-containlng promoter and similar concentrations are necessary for binding and transcrip-tional inhibition. Tallimustine shows strong selectivity by decreasing only correctly initiated transcripts. Even at high doses (20μM), however, they cannot disturb a competent pre-initiation complex or Pol II progression. 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The alkylating benzoyl mustard derivative tallimustine (FCE 24517) has powerfull anti-tumor activity. Using the electrophoretic mobility shift assay (EMSA) we determined that both compounds can prevent binding of TBP and, with 10-fold higher concentration, TBP-TFIIA (DA) and TBP-TRIA-TFIIB (DAB) to a TATA box. Once formed, the DA and DAB complexes are more resistant to MGB challenge. Both drugs can inhibit basal In vitro transcription of a minimal TATA-containlng promoter and similar concentrations are necessary for binding and transcrip-tional inhibition. Tallimustine shows strong selectivity by decreasing only correctly initiated transcripts. Even at high doses (20μM), however, they cannot disturb a competent pre-initiation complex or Pol II progression. This functional in vitro model will provide a way to investigate the activity of sequence-specific DNA binding drugs with potential anti-viral and anti-tumour activity and to develop novel more selective compounds.</description><subject>Antineoplastic Agents - pharmacology</subject><subject>Base Sequence</subject><subject>Biochemistry, Molecular Biology</subject><subject>Distamycins - pharmacology</subject><subject>DNA-Binding Proteins - drug effects</subject><subject>DNA-Binding Proteins - isolation & purification</subject><subject>DNA-Binding Proteins - metabolism</subject><subject>Humans</subject><subject>Intercalating Agents - pharmacology</subject><subject>Life Sciences</subject><subject>Molecular Sequence Data</subject><subject>Nitrogen Mustard Compounds - pharmacology</subject><subject>Oligodeoxyribonucleotides</subject><subject>Recombinant Proteins - metabolism</subject><subject>Saccharomyces cerevisiae - metabolism</subject><subject>TATA Box</subject><subject>TATA-Box Binding Protein</subject><subject>Transcription Factor TFIIA</subject><subject>Transcription Factor TFIIB</subject><subject>Transcription Factors - drug effects</subject><subject>Transcription Factors - isolation & purification</subject><subject>Transcription Factors - metabolism</subject><subject>Transcription, Genetic - drug effects</subject><issn>0305-1048</issn><issn>1362-4962</issn><fulltext>true</fulltext><rsrctype>article</rsrctype><creationdate>1995</creationdate><recordtype>article</recordtype><sourceid>EIF</sourceid><recordid>eNqFkk1vEzEQhi1EVULhyg1pT0gcNvX3x4FD2lJSKVIBFYS4WF6vtzHseoPtRO2_x2miiHLpxdbM-7z22DMAvEFwiqAip8HEU0ym25Az8QxMEOG4porj52ACCWQ1glS-AC9T-gUhoojRY3AshKSIywn4euFTNsO99aGaVSa0VTZ974d1yj64yoelb3yubs4-V40PrQ-3D1BjkumLWm18jmOVownJRr_KfgyvwFFn-uRe7_cT8O3y4835vF5cf7o6ny1qyyTNteLcQdQ6p1ypsFOMQUpwwyGjhLadVE6a1pZFYWs6W1IlzRl2girlbEtOwIfduat1M7iChlJGr1fRDybe69F4_VgJfqlvx40mkCski__9zr_8zzWfLfQ2B4kkUFCyQYV9t78rjn_WLmU9-GRd35vgxnXSQhAiMBJPgqi8E1FOnga5kEpyXMDpDrRxTCm67lArgno7ArqMgMbkISwjUAxv__2XA77vedHrnV467-4Osom_NRdEMD3_8VNfKKy-f5FKS_IX5W28Wg</recordid><startdate>19950525</startdate><enddate>19950525</enddate><creator>Bellorini, Marianna</creator><creator>Moncollin, Vincent</creator><creator>D'lncalci, Maurizio</creator><creator>Mongelli, Nicola</creator><creator>Mantovani, Roberto</creator><general>Oxford University Press</general><scope>BSCLL</scope><scope>CGR</scope><scope>CUY</scope><scope>CVF</scope><scope>ECM</scope><scope>EIF</scope><scope>NPM</scope><scope>AAYXX</scope><scope>CITATION</scope><scope>7TM</scope><scope>7U9</scope><scope>H94</scope><scope>7X8</scope><scope>1XC</scope><scope>5PM</scope></search><sort><creationdate>19950525</creationdate><title>Distamycin A and tallimustine inhibit TBP binding and basal in vitro transcription</title><author>Bellorini, Marianna ; Moncollin, Vincent ; D'lncalci, Maurizio ; Mongelli, Nicola ; Mantovani, Roberto</author></sort><facets><frbrtype>5</frbrtype><frbrgroupid>cdi_FETCH-LOGICAL-c584t-966e01dee9e104f9550432b605434df89e8adce8a92cafc4df34d652e7499ecd3</frbrgroupid><rsrctype>articles</rsrctype><prefilter>articles</prefilter><language>eng</language><creationdate>1995</creationdate><topic>Antineoplastic Agents - pharmacology</topic><topic>Base Sequence</topic><topic>Biochemistry, Molecular Biology</topic><topic>Distamycins - pharmacology</topic><topic>DNA-Binding Proteins - drug effects</topic><topic>DNA-Binding Proteins - isolation & purification</topic><topic>DNA-Binding Proteins - metabolism</topic><topic>Humans</topic><topic>Intercalating Agents - pharmacology</topic><topic>Life Sciences</topic><topic>Molecular Sequence Data</topic><topic>Nitrogen Mustard Compounds - pharmacology</topic><topic>Oligodeoxyribonucleotides</topic><topic>Recombinant Proteins - metabolism</topic><topic>Saccharomyces cerevisiae - metabolism</topic><topic>TATA Box</topic><topic>TATA-Box Binding Protein</topic><topic>Transcription Factor TFIIA</topic><topic>Transcription Factor TFIIB</topic><topic>Transcription Factors - drug effects</topic><topic>Transcription Factors - isolation & purification</topic><topic>Transcription Factors - metabolism</topic><topic>Transcription, Genetic - drug effects</topic><toplevel>peer_reviewed</toplevel><toplevel>online_resources</toplevel><creatorcontrib>Bellorini, Marianna</creatorcontrib><creatorcontrib>Moncollin, Vincent</creatorcontrib><creatorcontrib>D'lncalci, Maurizio</creatorcontrib><creatorcontrib>Mongelli, Nicola</creatorcontrib><creatorcontrib>Mantovani, Roberto</creatorcontrib><collection>Istex</collection><collection>Medline</collection><collection>MEDLINE</collection><collection>MEDLINE (Ovid)</collection><collection>MEDLINE</collection><collection>MEDLINE</collection><collection>PubMed</collection><collection>CrossRef</collection><collection>Nucleic Acids Abstracts</collection><collection>Virology and AIDS Abstracts</collection><collection>AIDS and Cancer Research Abstracts</collection><collection>MEDLINE - Academic</collection><collection>Hyper Article en Ligne (HAL)</collection><collection>PubMed Central (Full Participant titles)</collection><jtitle>Nucleic acids research</jtitle></facets><delivery><delcategory>Remote Search Resource</delcategory><fulltext>fulltext</fulltext></delivery><addata><au>Bellorini, Marianna</au><au>Moncollin, Vincent</au><au>D'lncalci, Maurizio</au><au>Mongelli, Nicola</au><au>Mantovani, Roberto</au><format>journal</format><genre>article</genre><ristype>JOUR</ristype><atitle>Distamycin A and tallimustine inhibit TBP binding and basal in vitro transcription</atitle><jtitle>Nucleic acids research</jtitle><addtitle>Nucleic Acids Res</addtitle><date>1995-05-25</date><risdate>1995</risdate><volume>23</volume><issue>10</issue><spage>1657</spage><epage>1663</epage><pages>1657-1663</pages><issn>0305-1048</issn><eissn>1362-4962</eissn><abstract>The antibiotic distamycin A is a DNA minor groove binding drug (MGB) that recognizes a stretch of a least four ATs. The alkylating benzoyl mustard derivative tallimustine (FCE 24517) has powerfull anti-tumor activity. Using the electrophoretic mobility shift assay (EMSA) we determined that both compounds can prevent binding of TBP and, with 10-fold higher concentration, TBP-TFIIA (DA) and TBP-TRIA-TFIIB (DAB) to a TATA box. Once formed, the DA and DAB complexes are more resistant to MGB challenge. Both drugs can inhibit basal In vitro transcription of a minimal TATA-containlng promoter and similar concentrations are necessary for binding and transcrip-tional inhibition. Tallimustine shows strong selectivity by decreasing only correctly initiated transcripts. Even at high doses (20μM), however, they cannot disturb a competent pre-initiation complex or Pol II progression. This functional in vitro model will provide a way to investigate the activity of sequence-specific DNA binding drugs with potential anti-viral and anti-tumour activity and to develop novel more selective compounds.</abstract><cop>England</cop><pub>Oxford University Press</pub><pmid>7784168</pmid><doi>10.1093/nar/23.10.1657</doi><tpages>7</tpages><oa>free_for_read</oa></addata></record> |
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| source | MEDLINE; Oxford University Press Journals Digital Archive Legacy; PubMed Central |
| subjects | Antineoplastic Agents - pharmacology Base Sequence Biochemistry, Molecular Biology Distamycins - pharmacology DNA-Binding Proteins - drug effects DNA-Binding Proteins - isolation & purification DNA-Binding Proteins - metabolism Humans Intercalating Agents - pharmacology Life Sciences Molecular Sequence Data Nitrogen Mustard Compounds - pharmacology Oligodeoxyribonucleotides Recombinant Proteins - metabolism Saccharomyces cerevisiae - metabolism TATA Box TATA-Box Binding Protein Transcription Factor TFIIA Transcription Factor TFIIB Transcription Factors - drug effects Transcription Factors - isolation & purification Transcription Factors - metabolism Transcription, Genetic - drug effects |
| title | Distamycin A and tallimustine inhibit TBP binding and basal in vitro transcription |
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