Novel synthetic molecules targeting the bacterial RNA polymerase assembly
Objectives: Despite extensive functional screening of the bacterial RNA polymerase (RNAP) over the past years, very few novel inhibitors have been reported. We have, therefore, decided to screen with a radically different, non-enzymic, protein–protein interaction assay. Our target is the highly cons...
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| Veröffentlicht in: | Journal of antimicrobial chemotherapy 2006-02, Vol.57 (2), p.245-251 |
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| container_title | Journal of antimicrobial chemotherapy |
| container_volume | 57 |
| creator | André, Estelle Bastide, Lionel Michaux-Charachon, Sylvie Gouby, Anne Villain-Guillot, Philippe Latouche, Jaqueline Bouchet, Aurélie Gualtiéri, Maxime Leonetti, Jean-Paul |
| description | Objectives: Despite extensive functional screening of the bacterial RNA polymerase (RNAP) over the past years, very few novel inhibitors have been reported. We have, therefore, decided to screen with a radically different, non-enzymic, protein–protein interaction assay. Our target is the highly conserved RNAP–σ interaction that is essential for transcription. Methods: Small molecule inhibitors of the RNAP–σ interaction were tested for their activity on transcription and on bacteria. Results: These compounds have antibacterial activity against Gram-positive bacteria including multiresistant clinical isolates. Conclusions: This is, to our knowledge, the first example of a small molecule inhibitor of this interaction. |
| doi_str_mv | 10.1093/jac/dki426 |
| format | Article |
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We have, therefore, decided to screen with a radically different, non-enzymic, protein–protein interaction assay. Our target is the highly conserved RNAP–σ interaction that is essential for transcription. Methods: Small molecule inhibitors of the RNAP–σ interaction were tested for their activity on transcription and on bacteria. Results: These compounds have antibacterial activity against Gram-positive bacteria including multiresistant clinical isolates. Conclusions: This is, to our knowledge, the first example of a small molecule inhibitor of this interaction.</description><identifier>ISSN: 0305-7453</identifier><identifier>EISSN: 1460-2091</identifier><identifier>DOI: 10.1093/jac/dki426</identifier><identifier>PMID: 16373430</identifier><identifier>CODEN: JACHDX</identifier><language>eng</language><publisher>Oxford: Oxford University Press</publisher><subject>Anti-Bacterial Agents - pharmacology ; anti-infective agents ; antibacterial drug screening ; antibacterials ; antibiotic resistance ; Antibiotics. Antiinfectious agents. Antiparasitic agents ; Bacillus anthracis - drug effects ; Bacillus cereus - drug effects ; Bacteria ; Bacteria - drug effects ; Bacteria - enzymology ; Biological and medical sciences ; DNA-Directed RNA Polymerases - drug effects ; Drug Resistance, Bacterial ; Enzyme-Linked Immunosorbent Assay ; Gram-Negative Bacteria - drug effects ; Gram-Positive Bacteria - drug effects ; Immunoprecipitation ; Medical sciences ; Microbial Sensitivity Tests ; Pharmacology. Drug treatments ; Staphylococcus epidermidis - drug effects ; Streptococcus pneumoniae - drug effects ; transcription ; Transcription, Genetic - drug effects</subject><ispartof>Journal of antimicrobial chemotherapy, 2006-02, Vol.57 (2), p.245-251</ispartof><rights>2006 INIST-CNRS</rights><rights>Copyright Oxford University Press(England) Feb 2006</rights><lds50>peer_reviewed</lds50><oa>free_for_read</oa><woscitedreferencessubscribed>false</woscitedreferencessubscribed><citedby>FETCH-LOGICAL-c447t-54a15250b5eb322c11946a0f77afb8c8c840c19ed912d90807706c25c717b3ff3</citedby><cites>FETCH-LOGICAL-c447t-54a15250b5eb322c11946a0f77afb8c8c840c19ed912d90807706c25c717b3ff3</cites></display><links><openurl>$$Topenurl_article</openurl><openurlfulltext>$$Topenurlfull_article</openurlfulltext><thumbnail>$$Tsyndetics_thumb_exl</thumbnail><link.rule.ids>314,776,780,27901,27902</link.rule.ids><backlink>$$Uhttp://pascal-francis.inist.fr/vibad/index.php?action=getRecordDetail&idt=17494015$$DView record in Pascal Francis$$Hfree_for_read</backlink><backlink>$$Uhttps://www.ncbi.nlm.nih.gov/pubmed/16373430$$D View this record in MEDLINE/PubMed$$Hfree_for_read</backlink></links><search><creatorcontrib>André, Estelle</creatorcontrib><creatorcontrib>Bastide, Lionel</creatorcontrib><creatorcontrib>Michaux-Charachon, Sylvie</creatorcontrib><creatorcontrib>Gouby, Anne</creatorcontrib><creatorcontrib>Villain-Guillot, Philippe</creatorcontrib><creatorcontrib>Latouche, Jaqueline</creatorcontrib><creatorcontrib>Bouchet, Aurélie</creatorcontrib><creatorcontrib>Gualtiéri, Maxime</creatorcontrib><creatorcontrib>Leonetti, Jean-Paul</creatorcontrib><title>Novel synthetic molecules targeting the bacterial RNA polymerase assembly</title><title>Journal of antimicrobial chemotherapy</title><addtitle>J. Antimicrob. Chemother</addtitle><description>Objectives: Despite extensive functional screening of the bacterial RNA polymerase (RNAP) over the past years, very few novel inhibitors have been reported. We have, therefore, decided to screen with a radically different, non-enzymic, protein–protein interaction assay. Our target is the highly conserved RNAP–σ interaction that is essential for transcription. Methods: Small molecule inhibitors of the RNAP–σ interaction were tested for their activity on transcription and on bacteria. Results: These compounds have antibacterial activity against Gram-positive bacteria including multiresistant clinical isolates. Conclusions: This is, to our knowledge, the first example of a small molecule inhibitor of this interaction.</description><subject>Anti-Bacterial Agents - pharmacology</subject><subject>anti-infective agents</subject><subject>antibacterial drug screening</subject><subject>antibacterials</subject><subject>antibiotic resistance</subject><subject>Antibiotics. Antiinfectious agents. Antiparasitic agents</subject><subject>Bacillus anthracis - drug effects</subject><subject>Bacillus cereus - drug effects</subject><subject>Bacteria</subject><subject>Bacteria - drug effects</subject><subject>Bacteria - enzymology</subject><subject>Biological and medical sciences</subject><subject>DNA-Directed RNA Polymerases - drug effects</subject><subject>Drug Resistance, Bacterial</subject><subject>Enzyme-Linked Immunosorbent Assay</subject><subject>Gram-Negative Bacteria - drug effects</subject><subject>Gram-Positive Bacteria - drug effects</subject><subject>Immunoprecipitation</subject><subject>Medical sciences</subject><subject>Microbial Sensitivity Tests</subject><subject>Pharmacology. Drug treatments</subject><subject>Staphylococcus epidermidis - drug effects</subject><subject>Streptococcus pneumoniae - drug effects</subject><subject>transcription</subject><subject>Transcription, Genetic - drug effects</subject><issn>0305-7453</issn><issn>1460-2091</issn><fulltext>true</fulltext><rsrctype>article</rsrctype><creationdate>2006</creationdate><recordtype>article</recordtype><sourceid>EIF</sourceid><recordid>eNqF0U1r3DAQBmARGpLNNpf-gGICzaHgZPRtH0NoN4FkSz9CQi9C1o4Tb2R7K9ml---rZZcGcik6CDQPI2ZeQt5ROKNQ8vOldeeL50YwtUcmVCjIGZT0DZkAB5lrIfkhOYpxCQBKquKAHFLFNRccJuR63v9Gn8V1Nzzh0Lis7T260WPMBhse01P3mKVSVlk3YGisz77NL7JV79ctBhsxszFiW_n1W7JfWx_xeHdPyd3nTz8ur_KbL7Pry4ub3Amhh1wKSyWTUEmsOGOO0lIoC7XWtq4Kl44AR0tclJQtSihAa1COSaeprnhd8yk53fZdhf7XiHEwbRMdem877MdoEi-ULOR_IQMmlEgLnJKTV3DZj6FLQxhGtdKMyk23j1vkQh9jwNqsQtPasDYUzCYGk2Iw2xgSfr_rOFYtLl7obu8JfNgBG531dbCda-KL06IUQDe_5lvXxAH__Kvb8GyU5lqaq4efZja_l19v6Xcz438BizGefw</recordid><startdate>20060201</startdate><enddate>20060201</enddate><creator>André, Estelle</creator><creator>Bastide, Lionel</creator><creator>Michaux-Charachon, Sylvie</creator><creator>Gouby, Anne</creator><creator>Villain-Guillot, Philippe</creator><creator>Latouche, Jaqueline</creator><creator>Bouchet, Aurélie</creator><creator>Gualtiéri, Maxime</creator><creator>Leonetti, Jean-Paul</creator><general>Oxford University Press</general><general>Oxford Publishing Limited (England)</general><scope>BSCLL</scope><scope>IQODW</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>7QL</scope><scope>7QO</scope><scope>7T7</scope><scope>7U7</scope><scope>7U9</scope><scope>8FD</scope><scope>C1K</scope><scope>FR3</scope><scope>H94</scope><scope>K9.</scope><scope>M7N</scope><scope>NAPCQ</scope><scope>P64</scope><scope>7X8</scope></search><sort><creationdate>20060201</creationdate><title>Novel synthetic molecules targeting the bacterial RNA polymerase assembly</title><author>André, Estelle ; Bastide, Lionel ; Michaux-Charachon, Sylvie ; Gouby, Anne ; Villain-Guillot, Philippe ; Latouche, Jaqueline ; Bouchet, Aurélie ; Gualtiéri, Maxime ; Leonetti, Jean-Paul</author></sort><facets><frbrtype>5</frbrtype><frbrgroupid>cdi_FETCH-LOGICAL-c447t-54a15250b5eb322c11946a0f77afb8c8c840c19ed912d90807706c25c717b3ff3</frbrgroupid><rsrctype>articles</rsrctype><prefilter>articles</prefilter><language>eng</language><creationdate>2006</creationdate><topic>Anti-Bacterial Agents - pharmacology</topic><topic>anti-infective agents</topic><topic>antibacterial drug screening</topic><topic>antibacterials</topic><topic>antibiotic resistance</topic><topic>Antibiotics. Antiinfectious agents. Antiparasitic agents</topic><topic>Bacillus anthracis - drug effects</topic><topic>Bacillus cereus - drug effects</topic><topic>Bacteria</topic><topic>Bacteria - drug effects</topic><topic>Bacteria - enzymology</topic><topic>Biological and medical sciences</topic><topic>DNA-Directed RNA Polymerases - drug effects</topic><topic>Drug Resistance, Bacterial</topic><topic>Enzyme-Linked Immunosorbent Assay</topic><topic>Gram-Negative Bacteria - drug effects</topic><topic>Gram-Positive Bacteria - drug effects</topic><topic>Immunoprecipitation</topic><topic>Medical sciences</topic><topic>Microbial Sensitivity Tests</topic><topic>Pharmacology. 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| subjects | Anti-Bacterial Agents - pharmacology anti-infective agents antibacterial drug screening antibacterials antibiotic resistance Antibiotics. Antiinfectious agents. Antiparasitic agents Bacillus anthracis - drug effects Bacillus cereus - drug effects Bacteria Bacteria - drug effects Bacteria - enzymology Biological and medical sciences DNA-Directed RNA Polymerases - drug effects Drug Resistance, Bacterial Enzyme-Linked Immunosorbent Assay Gram-Negative Bacteria - drug effects Gram-Positive Bacteria - drug effects Immunoprecipitation Medical sciences Microbial Sensitivity Tests Pharmacology. Drug treatments Staphylococcus epidermidis - drug effects Streptococcus pneumoniae - drug effects transcription Transcription, Genetic - drug effects |
| title | Novel synthetic molecules targeting the bacterial RNA polymerase assembly |
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