Selective small molecule inhibitors of the potential breast cancer marker, human arylamine N-acetyltransferase 1, and its murine homologue, mouse arylamine N-acetyltransferase 2
The identification, synthesis and evaluation of a series of rhodanine and thiazolidin-2,4-dione derivatives as selective inhibitors of human arylamine N-acetyltransferase 1 and mouse arylamine N-acetyltransferase 2 is described. The identification, synthesis and evaluation of a series of rhodanine a...
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| Veröffentlicht in: | Bioorganic & medicinal chemistry 2009-01, Vol.17 (2), p.905-918 |
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| container_title | Bioorganic & medicinal chemistry |
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| creator | Russell, Angela J. Westwood, Isaac M. Crawford, Matthew H.J. Robinson, James Kawamura, Akane Redfield, Christina Laurieri, Nicola Lowe, Edward D. Davies, Stephen G. Sim, Edith |
| description | The identification, synthesis and evaluation of a series of rhodanine and thiazolidin-2,4-dione derivatives as selective inhibitors of human arylamine
N-acetyltransferase 1 and mouse arylamine
N-acetyltransferase 2 is described.
The identification, synthesis and evaluation of a series of rhodanine and thiazolidin-2,4-dione derivatives as selective inhibitors of human arylamine
N-acetyltransferase 1 and mouse arylamine
N-acetyltransferase 2 is described. The most potent inhibitors identified have submicromolar activity and inhibit both the recombinant proteins and human NAT1 in ZR-75 cell lysates in a competitive manner.
1H NMR studies on purified mouse Nat2 demonstrate that the inhibitors bind within the putative active site of the enzyme. |
| doi_str_mv | 10.1016/j.bmc.2008.11.032 |
| format | Article |
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N-acetyltransferase 1 and mouse arylamine
N-acetyltransferase 2 is described.
The identification, synthesis and evaluation of a series of rhodanine and thiazolidin-2,4-dione derivatives as selective inhibitors of human arylamine
N-acetyltransferase 1 and mouse arylamine
N-acetyltransferase 2 is described. The most potent inhibitors identified have submicromolar activity and inhibit both the recombinant proteins and human NAT1 in ZR-75 cell lysates in a competitive manner.
1H NMR studies on purified mouse Nat2 demonstrate that the inhibitors bind within the putative active site of the enzyme.</description><identifier>ISSN: 0968-0896</identifier><identifier>EISSN: 1464-3391</identifier><identifier>DOI: 10.1016/j.bmc.2008.11.032</identifier><identifier>PMID: 19059786</identifier><language>eng</language><publisher>Amsterdam: Elsevier Ltd</publisher><subject>Animals ; Arylamine N-acetyltransferase ; Arylamine N-Acetyltransferase - antagonists & inhibitors ; Binding Sites ; Biological and medical sciences ; Biomarkers, Tumor - antagonists & inhibitors ; Breast cancer ; Breast Neoplasms - drug therapy ; Breast Neoplasms - pathology ; Enzyme Inhibitors ; Female ; Host-tumor relations. Immunology. Biological markers ; Humans ; Isoenzymes - antagonists & inhibitors ; Medical sciences ; Mice ; Miscellaneous ; Pharmacology. Drug treatments ; Rhodanine ; Rhodanine - chemical synthesis ; Rhodanine - pharmacology ; Thiazolidin-2,4-dione ; Thiazolidinediones - chemical synthesis ; Thiazolidinediones - pharmacology ; Tumors</subject><ispartof>Bioorganic & medicinal chemistry, 2009-01, Vol.17 (2), p.905-918</ispartof><rights>2008 Elsevier Ltd</rights><rights>2009 INIST-CNRS</rights><lds50>peer_reviewed</lds50><woscitedreferencessubscribed>false</woscitedreferencessubscribed><citedby>FETCH-LOGICAL-c478t-b6b5777c42d886e9173c78f6db4357c752d8c4e331f09b014883d132a2a70ab23</citedby><cites>FETCH-LOGICAL-c478t-b6b5777c42d886e9173c78f6db4357c752d8c4e331f09b014883d132a2a70ab23</cites></display><links><openurl>$$Topenurl_article</openurl><openurlfulltext>$$Topenurlfull_article</openurlfulltext><thumbnail>$$Tsyndetics_thumb_exl</thumbnail><linktohtml>$$Uhttps://dx.doi.org/10.1016/j.bmc.2008.11.032$$EHTML$$P50$$Gelsevier$$H</linktohtml><link.rule.ids>314,780,784,3550,27924,27925,45995</link.rule.ids><backlink>$$Uhttp://pascal-francis.inist.fr/vibad/index.php?action=getRecordDetail&idt=21127129$$DView record in Pascal Francis$$Hfree_for_read</backlink><backlink>$$Uhttps://www.ncbi.nlm.nih.gov/pubmed/19059786$$D View this record in MEDLINE/PubMed$$Hfree_for_read</backlink></links><search><creatorcontrib>Russell, Angela J.</creatorcontrib><creatorcontrib>Westwood, Isaac M.</creatorcontrib><creatorcontrib>Crawford, Matthew H.J.</creatorcontrib><creatorcontrib>Robinson, James</creatorcontrib><creatorcontrib>Kawamura, Akane</creatorcontrib><creatorcontrib>Redfield, Christina</creatorcontrib><creatorcontrib>Laurieri, Nicola</creatorcontrib><creatorcontrib>Lowe, Edward D.</creatorcontrib><creatorcontrib>Davies, Stephen G.</creatorcontrib><creatorcontrib>Sim, Edith</creatorcontrib><title>Selective small molecule inhibitors of the potential breast cancer marker, human arylamine N-acetyltransferase 1, and its murine homologue, mouse arylamine N-acetyltransferase 2</title><title>Bioorganic & medicinal chemistry</title><addtitle>Bioorg Med Chem</addtitle><description>The identification, synthesis and evaluation of a series of rhodanine and thiazolidin-2,4-dione derivatives as selective inhibitors of human arylamine
N-acetyltransferase 1 and mouse arylamine
N-acetyltransferase 2 is described.
The identification, synthesis and evaluation of a series of rhodanine and thiazolidin-2,4-dione derivatives as selective inhibitors of human arylamine
N-acetyltransferase 1 and mouse arylamine
N-acetyltransferase 2 is described. The most potent inhibitors identified have submicromolar activity and inhibit both the recombinant proteins and human NAT1 in ZR-75 cell lysates in a competitive manner.
1H NMR studies on purified mouse Nat2 demonstrate that the inhibitors bind within the putative active site of the enzyme.</description><subject>Animals</subject><subject>Arylamine N-acetyltransferase</subject><subject>Arylamine N-Acetyltransferase - antagonists & inhibitors</subject><subject>Binding Sites</subject><subject>Biological and medical sciences</subject><subject>Biomarkers, Tumor - antagonists & inhibitors</subject><subject>Breast cancer</subject><subject>Breast Neoplasms - drug therapy</subject><subject>Breast Neoplasms - pathology</subject><subject>Enzyme Inhibitors</subject><subject>Female</subject><subject>Host-tumor relations. Immunology. Biological markers</subject><subject>Humans</subject><subject>Isoenzymes - antagonists & inhibitors</subject><subject>Medical sciences</subject><subject>Mice</subject><subject>Miscellaneous</subject><subject>Pharmacology. Drug treatments</subject><subject>Rhodanine</subject><subject>Rhodanine - chemical synthesis</subject><subject>Rhodanine - pharmacology</subject><subject>Thiazolidin-2,4-dione</subject><subject>Thiazolidinediones - chemical synthesis</subject><subject>Thiazolidinediones - pharmacology</subject><subject>Tumors</subject><issn>0968-0896</issn><issn>1464-3391</issn><fulltext>true</fulltext><rsrctype>article</rsrctype><creationdate>2009</creationdate><recordtype>article</recordtype><sourceid>EIF</sourceid><recordid>eNqFks2OFCEUhYnROO3oA7gxbHTV1XKBBiquzMS_ZKILdU0o6pZNS1W1QE3Sj-UbSqc7uhtXBPLdc0_OgZDnwDbAQL3eb7rRbzhjZgOwYYI_ICuQSjZCtPCQrFirTMNMq67Ik5z3jDEuW3hMrqBl21YbtSK_v2JEX8Id0jy6GOk41_sSkYZpF7pQ5pTpPNCyQ3qYC04luEi7hC4X6t3kMdHRpZ-Y1nS3jG6iLh2jG8OE9HPjPJZjLMlNecDkMlJYUzf1NJRMxyWdqN1cV84_FlzX3UtF7hfgT8mjwcWMzy7nNfn-_t23m4_N7ZcPn27e3jZealOaTnVbrbWXvDdGYQtaeG0G1XdSbLXX2_ruJQoBA2s7BtIY0YPgjjvNXMfFNXl11j2k-deCudgxZI8xugmrT6uUkRyA_RfkTEjDlKognEGf5pwTDvaQQg3vaIHZU6F2b2uh9lSoBbC10Drz4iK-dCP2_yYuDVbg5QVw2bs41Kh8yH-56pBr4G3l3pw5rJndBUw2-4C1vz6k-gFsP4d7bPwB-87Aow</recordid><startdate>20090115</startdate><enddate>20090115</enddate><creator>Russell, Angela J.</creator><creator>Westwood, Isaac M.</creator><creator>Crawford, Matthew H.J.</creator><creator>Robinson, James</creator><creator>Kawamura, Akane</creator><creator>Redfield, Christina</creator><creator>Laurieri, Nicola</creator><creator>Lowe, Edward D.</creator><creator>Davies, Stephen G.</creator><creator>Sim, Edith</creator><general>Elsevier Ltd</general><general>Elsevier</general><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>7QO</scope><scope>8FD</scope><scope>FR3</scope><scope>P64</scope><scope>7X8</scope></search><sort><creationdate>20090115</creationdate><title>Selective small molecule inhibitors of the potential breast cancer marker, human arylamine N-acetyltransferase 1, and its murine homologue, mouse arylamine N-acetyltransferase 2</title><author>Russell, Angela J. ; Westwood, Isaac M. ; Crawford, Matthew H.J. ; Robinson, James ; Kawamura, Akane ; Redfield, Christina ; Laurieri, Nicola ; Lowe, Edward D. ; Davies, Stephen G. ; Sim, Edith</author></sort><facets><frbrtype>5</frbrtype><frbrgroupid>cdi_FETCH-LOGICAL-c478t-b6b5777c42d886e9173c78f6db4357c752d8c4e331f09b014883d132a2a70ab23</frbrgroupid><rsrctype>articles</rsrctype><prefilter>articles</prefilter><language>eng</language><creationdate>2009</creationdate><topic>Animals</topic><topic>Arylamine N-acetyltransferase</topic><topic>Arylamine N-Acetyltransferase - antagonists & inhibitors</topic><topic>Binding Sites</topic><topic>Biological and medical sciences</topic><topic>Biomarkers, Tumor - antagonists & inhibitors</topic><topic>Breast cancer</topic><topic>Breast Neoplasms - drug therapy</topic><topic>Breast Neoplasms - pathology</topic><topic>Enzyme Inhibitors</topic><topic>Female</topic><topic>Host-tumor relations. Immunology. Biological markers</topic><topic>Humans</topic><topic>Isoenzymes - antagonists & inhibitors</topic><topic>Medical sciences</topic><topic>Mice</topic><topic>Miscellaneous</topic><topic>Pharmacology. Drug treatments</topic><topic>Rhodanine</topic><topic>Rhodanine - chemical synthesis</topic><topic>Rhodanine - pharmacology</topic><topic>Thiazolidin-2,4-dione</topic><topic>Thiazolidinediones - chemical synthesis</topic><topic>Thiazolidinediones - pharmacology</topic><topic>Tumors</topic><toplevel>peer_reviewed</toplevel><toplevel>online_resources</toplevel><creatorcontrib>Russell, Angela J.</creatorcontrib><creatorcontrib>Westwood, Isaac M.</creatorcontrib><creatorcontrib>Crawford, Matthew H.J.</creatorcontrib><creatorcontrib>Robinson, James</creatorcontrib><creatorcontrib>Kawamura, Akane</creatorcontrib><creatorcontrib>Redfield, Christina</creatorcontrib><creatorcontrib>Laurieri, Nicola</creatorcontrib><creatorcontrib>Lowe, Edward D.</creatorcontrib><creatorcontrib>Davies, Stephen G.</creatorcontrib><creatorcontrib>Sim, Edith</creatorcontrib><collection>Pascal-Francis</collection><collection>Medline</collection><collection>MEDLINE</collection><collection>MEDLINE (Ovid)</collection><collection>MEDLINE</collection><collection>MEDLINE</collection><collection>PubMed</collection><collection>CrossRef</collection><collection>Biotechnology Research Abstracts</collection><collection>Technology Research Database</collection><collection>Engineering Research Database</collection><collection>Biotechnology and BioEngineering Abstracts</collection><collection>MEDLINE - Academic</collection><jtitle>Bioorganic & medicinal chemistry</jtitle></facets><delivery><delcategory>Remote Search Resource</delcategory><fulltext>fulltext</fulltext></delivery><addata><au>Russell, Angela J.</au><au>Westwood, Isaac M.</au><au>Crawford, Matthew H.J.</au><au>Robinson, James</au><au>Kawamura, Akane</au><au>Redfield, Christina</au><au>Laurieri, Nicola</au><au>Lowe, Edward D.</au><au>Davies, Stephen G.</au><au>Sim, Edith</au><format>journal</format><genre>article</genre><ristype>JOUR</ristype><atitle>Selective small molecule inhibitors of the potential breast cancer marker, human arylamine N-acetyltransferase 1, and its murine homologue, mouse arylamine N-acetyltransferase 2</atitle><jtitle>Bioorganic & medicinal chemistry</jtitle><addtitle>Bioorg Med Chem</addtitle><date>2009-01-15</date><risdate>2009</risdate><volume>17</volume><issue>2</issue><spage>905</spage><epage>918</epage><pages>905-918</pages><issn>0968-0896</issn><eissn>1464-3391</eissn><abstract>The identification, synthesis and evaluation of a series of rhodanine and thiazolidin-2,4-dione derivatives as selective inhibitors of human arylamine
N-acetyltransferase 1 and mouse arylamine
N-acetyltransferase 2 is described.
The identification, synthesis and evaluation of a series of rhodanine and thiazolidin-2,4-dione derivatives as selective inhibitors of human arylamine
N-acetyltransferase 1 and mouse arylamine
N-acetyltransferase 2 is described. The most potent inhibitors identified have submicromolar activity and inhibit both the recombinant proteins and human NAT1 in ZR-75 cell lysates in a competitive manner.
1H NMR studies on purified mouse Nat2 demonstrate that the inhibitors bind within the putative active site of the enzyme.</abstract><cop>Amsterdam</cop><pub>Elsevier Ltd</pub><pmid>19059786</pmid><doi>10.1016/j.bmc.2008.11.032</doi><tpages>14</tpages></addata></record> |
| fulltext | fulltext |
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| ispartof | Bioorganic & medicinal chemistry, 2009-01, Vol.17 (2), p.905-918 |
| issn | 0968-0896 1464-3391 |
| language | eng |
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| source | MEDLINE; Elsevier ScienceDirect Journals Complete |
| subjects | Animals Arylamine N-acetyltransferase Arylamine N-Acetyltransferase - antagonists & inhibitors Binding Sites Biological and medical sciences Biomarkers, Tumor - antagonists & inhibitors Breast cancer Breast Neoplasms - drug therapy Breast Neoplasms - pathology Enzyme Inhibitors Female Host-tumor relations. Immunology. Biological markers Humans Isoenzymes - antagonists & inhibitors Medical sciences Mice Miscellaneous Pharmacology. Drug treatments Rhodanine Rhodanine - chemical synthesis Rhodanine - pharmacology Thiazolidin-2,4-dione Thiazolidinediones - chemical synthesis Thiazolidinediones - pharmacology Tumors |
| title | Selective small molecule inhibitors of the potential breast cancer marker, human arylamine N-acetyltransferase 1, and its murine homologue, mouse arylamine N-acetyltransferase 2 |
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