Structure-Activity Relationships for Non-Steroidal Inhibitors of Aromatase
Abstract A model is described for the binding of non-steroidal inhibitors of aromatase to the enzyme with interaction of a ligand with the Fe3+-haem of the cytochrome. The model suggests that the inhibitors utilise a common binding site with ring A of the steroidal substrates.
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| Veröffentlicht in: | Journal of enzyme inhibition 1988, Vol.2 (3), p.215-229 |
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| container_end_page | 229 |
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| container_issue | 3 |
| container_start_page | 215 |
| container_title | Journal of enzyme inhibition |
| container_volume | 2 |
| creator | Banting, L. Smith, H. J. James, M. Jones, G. Nazareth, W. Nicholls, P. J. Hewlins, M. J. E. Rowlands, M. G. |
| description | Abstract
A model is described for the binding of non-steroidal inhibitors of aromatase to the enzyme with interaction of a ligand with the Fe3+-haem of the cytochrome. The model suggests that the inhibitors utilise a common binding site with ring A of the steroidal substrates. |
| doi_str_mv | 10.3109/14756368809040728 |
| format | Article |
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A model is described for the binding of non-steroidal inhibitors of aromatase to the enzyme with interaction of a ligand with the Fe3+-haem of the cytochrome. The model suggests that the inhibitors utilise a common binding site with ring A of the steroidal substrates.</description><identifier>ISSN: 1475-6366</identifier><identifier>ISSN: 8755-5093</identifier><identifier>EISSN: 1475-6374</identifier><identifier>DOI: 10.3109/14756368809040728</identifier><identifier>PMID: 3241182</identifier><language>eng</language><publisher>Switzerland: Informa UK Ltd</publisher><subject>aminoglutethimide ; androsten-dedione ; Androstenedione - analogs & derivatives ; Androstenedione - chemical synthesis ; Androstenedione - pharmacology ; Aromatase ; Aromatase Inhibitors ; Binding Sites ; Cholesterol Side-Chain Cleavage Enzyme - antagonists & inhibitors ; Computer Simulation ; Female ; Humans ; Kinetics ; Models, Molecular ; Molecular Conformation ; Molecular Structure ; Placenta - enzymology ; Pregnancy ; reversible inhibitors ; structure-activity ; Structure-Activity Relationship</subject><ispartof>Journal of enzyme inhibition, 1988, Vol.2 (3), p.215-229</ispartof><rights>1988 Informa UK Ltd All rights reserved: reproduction in whole or part not permitted 1988</rights><lds50>peer_reviewed</lds50><woscitedreferencessubscribed>false</woscitedreferencessubscribed><citedby>FETCH-LOGICAL-c316t-feb0430831e95cd788baef79c027057082c1ecd63161dde55503a776c118081e3</citedby><cites>FETCH-LOGICAL-c316t-feb0430831e95cd788baef79c027057082c1ecd63161dde55503a776c118081e3</cites></display><links><openurl>$$Topenurl_article</openurl><openurlfulltext>$$Topenurlfull_article</openurlfulltext><thumbnail>$$Tsyndetics_thumb_exl</thumbnail><linktopdf>$$Uhttps://www.tandfonline.com/doi/pdf/10.3109/14756368809040728$$EPDF$$P50$$Ginformahealthcare$$H</linktopdf><linktohtml>$$Uhttps://www.tandfonline.com/doi/full/10.3109/14756368809040728$$EHTML$$P50$$Ginformahealthcare$$H</linktohtml><link.rule.ids>314,777,781,4010,27904,27905,27906,61200,61381</link.rule.ids><backlink>$$Uhttps://www.ncbi.nlm.nih.gov/pubmed/3241182$$D View this record in MEDLINE/PubMed$$Hfree_for_read</backlink></links><search><creatorcontrib>Banting, L.</creatorcontrib><creatorcontrib>Smith, H. J.</creatorcontrib><creatorcontrib>James, M.</creatorcontrib><creatorcontrib>Jones, G.</creatorcontrib><creatorcontrib>Nazareth, W.</creatorcontrib><creatorcontrib>Nicholls, P. J.</creatorcontrib><creatorcontrib>Hewlins, M. J. E.</creatorcontrib><creatorcontrib>Rowlands, M. G.</creatorcontrib><title>Structure-Activity Relationships for Non-Steroidal Inhibitors of Aromatase</title><title>Journal of enzyme inhibition</title><addtitle>J Enzyme Inhib</addtitle><description>Abstract
A model is described for the binding of non-steroidal inhibitors of aromatase to the enzyme with interaction of a ligand with the Fe3+-haem of the cytochrome. The model suggests that the inhibitors utilise a common binding site with ring A of the steroidal substrates.</description><subject>aminoglutethimide</subject><subject>androsten-dedione</subject><subject>Androstenedione - analogs & derivatives</subject><subject>Androstenedione - chemical synthesis</subject><subject>Androstenedione - pharmacology</subject><subject>Aromatase</subject><subject>Aromatase Inhibitors</subject><subject>Binding Sites</subject><subject>Cholesterol Side-Chain Cleavage Enzyme - antagonists & inhibitors</subject><subject>Computer Simulation</subject><subject>Female</subject><subject>Humans</subject><subject>Kinetics</subject><subject>Models, Molecular</subject><subject>Molecular Conformation</subject><subject>Molecular Structure</subject><subject>Placenta - enzymology</subject><subject>Pregnancy</subject><subject>reversible inhibitors</subject><subject>structure-activity</subject><subject>Structure-Activity Relationship</subject><issn>1475-6366</issn><issn>8755-5093</issn><issn>1475-6374</issn><fulltext>true</fulltext><rsrctype>article</rsrctype><creationdate>1988</creationdate><recordtype>article</recordtype><sourceid>EIF</sourceid><recordid>eNp9kF9LwzAUxYMoc04_gA9Cn3yrJk2bZOjLGP6ZDAWnzyFNb2lG28wkVfbt7dgYiOjTvdx7zuHwQ-ic4CtK8PiapDxjlAmBxzjFPBEHaLi5xYzy9HC_M3aMTrxfYpyQhKQDNKBJSohIhuhpEVynQ-cgnuhgPk1YR69Qq2Bs6yuz8lFpXfRs23gRwFlTqDqatZXJTbDOR7aMJs42KigPp-ioVLWHs90coff7u7fpYzx_eZhNJ_NYU8JCXEKOU4oFJTDOdMGFyBWUfKxxwnHGsUg0AV2wXkyKArIsw1RxznRfGAsCdIQut7krZz868EE2xmuoa9WC7bzkghOWpbwXkq1QO-u9g1KunGmUW0uC5Yaf_MWv91zswru8gWLv2AHr_7fbv2l7MI36sq4uZFDr2rrSqVYbv4n-O_7mh70CVYdKKwdyaTvX9tz-KfcNOwyP7w</recordid><startdate>1988</startdate><enddate>1988</enddate><creator>Banting, L.</creator><creator>Smith, H. J.</creator><creator>James, M.</creator><creator>Jones, G.</creator><creator>Nazareth, W.</creator><creator>Nicholls, P. J.</creator><creator>Hewlins, M. J. E.</creator><creator>Rowlands, M. G.</creator><general>Informa UK Ltd</general><general>Taylor & Francis</general><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>7X8</scope></search><sort><creationdate>1988</creationdate><title>Structure-Activity Relationships for Non-Steroidal Inhibitors of Aromatase</title><author>Banting, L. ; Smith, H. J. ; James, M. ; Jones, G. ; Nazareth, W. ; Nicholls, P. J. ; Hewlins, M. J. E. ; Rowlands, M. 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J.</creatorcontrib><creatorcontrib>James, M.</creatorcontrib><creatorcontrib>Jones, G.</creatorcontrib><creatorcontrib>Nazareth, W.</creatorcontrib><creatorcontrib>Nicholls, P. J.</creatorcontrib><creatorcontrib>Hewlins, M. J. E.</creatorcontrib><creatorcontrib>Rowlands, M. G.</creatorcontrib><collection>Medline</collection><collection>MEDLINE</collection><collection>MEDLINE (Ovid)</collection><collection>MEDLINE</collection><collection>MEDLINE</collection><collection>PubMed</collection><collection>CrossRef</collection><collection>MEDLINE - Academic</collection><jtitle>Journal of enzyme inhibition</jtitle></facets><delivery><delcategory>Remote Search Resource</delcategory><fulltext>fulltext</fulltext></delivery><addata><au>Banting, L.</au><au>Smith, H. J.</au><au>James, M.</au><au>Jones, G.</au><au>Nazareth, W.</au><au>Nicholls, P. J.</au><au>Hewlins, M. J. E.</au><au>Rowlands, M. G.</au><format>journal</format><genre>article</genre><ristype>JOUR</ristype><atitle>Structure-Activity Relationships for Non-Steroidal Inhibitors of Aromatase</atitle><jtitle>Journal of enzyme inhibition</jtitle><addtitle>J Enzyme Inhib</addtitle><date>1988</date><risdate>1988</risdate><volume>2</volume><issue>3</issue><spage>215</spage><epage>229</epage><pages>215-229</pages><issn>1475-6366</issn><issn>8755-5093</issn><eissn>1475-6374</eissn><abstract>Abstract
A model is described for the binding of non-steroidal inhibitors of aromatase to the enzyme with interaction of a ligand with the Fe3+-haem of the cytochrome. The model suggests that the inhibitors utilise a common binding site with ring A of the steroidal substrates.</abstract><cop>Switzerland</cop><pub>Informa UK Ltd</pub><pmid>3241182</pmid><doi>10.3109/14756368809040728</doi><tpages>15</tpages></addata></record> |
| fulltext | fulltext |
| identifier | ISSN: 1475-6366 |
| ispartof | Journal of enzyme inhibition, 1988, Vol.2 (3), p.215-229 |
| issn | 1475-6366 8755-5093 1475-6374 |
| language | eng |
| recordid | cdi_proquest_miscellaneous_78716547 |
| source | MEDLINE; Taylor & Francis:Master (3349 titles); Alma/SFX Local Collection |
| subjects | aminoglutethimide androsten-dedione Androstenedione - analogs & derivatives Androstenedione - chemical synthesis Androstenedione - pharmacology Aromatase Aromatase Inhibitors Binding Sites Cholesterol Side-Chain Cleavage Enzyme - antagonists & inhibitors Computer Simulation Female Humans Kinetics Models, Molecular Molecular Conformation Molecular Structure Placenta - enzymology Pregnancy reversible inhibitors structure-activity Structure-Activity Relationship |
| title | Structure-Activity Relationships for Non-Steroidal Inhibitors of Aromatase |
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