Biochemical mode of action and differential activity of new ecdysone agonists against mosquitoes and moths
THQ (1-aroyl-4-(arylamino)-1,2,3,4-tetrahydroquinoline) compounds were identified by FMC Corporation in cell-based assays that used ecdysone receptors from Drosophila melanogaster, Heliothis virescens, or Plodia interpunctata. THQ compounds showed weak insecticidal activity against H. virescens and,...
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| Veröffentlicht in: | Archives of insect biochemistry and physiology 2005-04, Vol.58 (4), p.234-242 |
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| creator | Palli, S.R Tice, C.M Margam, V.M Clark, A.M |
| description | THQ (1-aroyl-4-(arylamino)-1,2,3,4-tetrahydroquinoline) compounds were identified by FMC Corporation in cell-based assays that used ecdysone receptors from Drosophila melanogaster, Heliothis virescens, or Plodia interpunctata. THQ compounds showed weak insecticidal activity against H. virescens and, therefore, were not developed further. Several ecdysone agonists based on THQ chemotype have been synthesized and tested for their activity against a number of EcRs in transactivation assays. The THQ compound, RG-120768, activated AaEcR (EcR from A. aegypti) but did not activate EcRs cloned from other insects. In transactivation assays, all six THQ ligands tested functioned through AaEcR but not through CfEcR (EcR from Choristoneura fumiferana). Three THQ compounds that showed higher activity in transactivation assays were tested in tobacco bud moth, H. virescens, and yellow fever mosquito, A. aegypti. These compounds showed higher activity in A. aegypti when compared to their activity in H. virescens. These data show that the THQ ligands are a new class of non-steroidal ecdysone agonists with preferential activity against mosquitoes. |
| doi_str_mv | 10.1002/arch.20046 |
| format | Article |
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THQ compounds showed weak insecticidal activity against H. virescens and, therefore, were not developed further. Several ecdysone agonists based on THQ chemotype have been synthesized and tested for their activity against a number of EcRs in transactivation assays. The THQ compound, RG-120768, activated AaEcR (EcR from A. aegypti) but did not activate EcRs cloned from other insects. In transactivation assays, all six THQ ligands tested functioned through AaEcR but not through CfEcR (EcR from Choristoneura fumiferana). Three THQ compounds that showed higher activity in transactivation assays were tested in tobacco bud moth, H. virescens, and yellow fever mosquito, A. aegypti. These compounds showed higher activity in A. aegypti when compared to their activity in H. virescens. These data show that the THQ ligands are a new class of non-steroidal ecdysone agonists with preferential activity against mosquitoes.</description><identifier>ISSN: 0739-4462</identifier><identifier>EISSN: 1520-6327</identifier><identifier>DOI: 10.1002/arch.20046</identifier><identifier>PMID: 15756700</identifier><language>eng</language><publisher>Hoboken: Wiley Subscription Services, Inc., A Wiley Company</publisher><subject>3T3 Cells ; Aedes ; Aedes aegypti ; Aminoquinolines - chemistry ; Aminoquinolines - pharmacology ; Animals ; bioassays ; Choristoneura fumiferana ; Cloning, Molecular ; Culicidae ; diacylhydrazine ; Drosophila melanogaster ; ecdysone agonists ; ecdysone receptor ; ecdysone receptors ; Heliothis ; Heliothis virescens ; hormone receptors ; insecticidal properties ; Insecticides - pharmacology ; mechanism of action ; Mice ; mortality ; mosquito ; mosquito control ; Moths ; Noctuidae ; Plodia interpunctata ; quinolines ; Receptors, Steroid - agonists ; Receptors, Steroid - genetics ; Species Specificity ; tetrahydroquinoline ; toxicity ; Transcriptional Activation</subject><ispartof>Archives of insect biochemistry and physiology, 2005-04, Vol.58 (4), p.234-242</ispartof><rights>Copyright © 2005 Wiley‐Liss, Inc.</rights><rights>Copyright 2005 Wiley-Liss, Inc.</rights><lds50>peer_reviewed</lds50><woscitedreferencessubscribed>false</woscitedreferencessubscribed><citedby>FETCH-LOGICAL-c4866-c513a79e2d1d73ffb62e311bcfbcfa798f3cf870895b964bfa5bc858aeff24f33</citedby><cites>FETCH-LOGICAL-c4866-c513a79e2d1d73ffb62e311bcfbcfa798f3cf870895b964bfa5bc858aeff24f33</cites></display><links><openurl>$$Topenurl_article</openurl><openurlfulltext>$$Topenurlfull_article</openurlfulltext><thumbnail>$$Tsyndetics_thumb_exl</thumbnail><linktopdf>$$Uhttps://onlinelibrary.wiley.com/doi/pdf/10.1002%2Farch.20046$$EPDF$$P50$$Gwiley$$H</linktopdf><linktohtml>$$Uhttps://onlinelibrary.wiley.com/doi/full/10.1002%2Farch.20046$$EHTML$$P50$$Gwiley$$H</linktohtml><link.rule.ids>314,780,784,1417,27924,27925,45574,45575</link.rule.ids><backlink>$$Uhttps://www.ncbi.nlm.nih.gov/pubmed/15756700$$D View this record in MEDLINE/PubMed$$Hfree_for_read</backlink></links><search><creatorcontrib>Palli, S.R</creatorcontrib><creatorcontrib>Tice, C.M</creatorcontrib><creatorcontrib>Margam, V.M</creatorcontrib><creatorcontrib>Clark, A.M</creatorcontrib><title>Biochemical mode of action and differential activity of new ecdysone agonists against mosquitoes and moths</title><title>Archives of insect biochemistry and physiology</title><addtitle>Arch. Insect Biochem. Physiol</addtitle><description>THQ (1-aroyl-4-(arylamino)-1,2,3,4-tetrahydroquinoline) compounds were identified by FMC Corporation in cell-based assays that used ecdysone receptors from Drosophila melanogaster, Heliothis virescens, or Plodia interpunctata. THQ compounds showed weak insecticidal activity against H. virescens and, therefore, were not developed further. Several ecdysone agonists based on THQ chemotype have been synthesized and tested for their activity against a number of EcRs in transactivation assays. The THQ compound, RG-120768, activated AaEcR (EcR from A. aegypti) but did not activate EcRs cloned from other insects. In transactivation assays, all six THQ ligands tested functioned through AaEcR but not through CfEcR (EcR from Choristoneura fumiferana). Three THQ compounds that showed higher activity in transactivation assays were tested in tobacco bud moth, H. virescens, and yellow fever mosquito, A. aegypti. These compounds showed higher activity in A. aegypti when compared to their activity in H. virescens. These data show that the THQ ligands are a new class of non-steroidal ecdysone agonists with preferential activity against mosquitoes.</description><subject>3T3 Cells</subject><subject>Aedes</subject><subject>Aedes aegypti</subject><subject>Aminoquinolines - chemistry</subject><subject>Aminoquinolines - pharmacology</subject><subject>Animals</subject><subject>bioassays</subject><subject>Choristoneura fumiferana</subject><subject>Cloning, Molecular</subject><subject>Culicidae</subject><subject>diacylhydrazine</subject><subject>Drosophila melanogaster</subject><subject>ecdysone agonists</subject><subject>ecdysone receptor</subject><subject>ecdysone receptors</subject><subject>Heliothis</subject><subject>Heliothis virescens</subject><subject>hormone receptors</subject><subject>insecticidal properties</subject><subject>Insecticides - pharmacology</subject><subject>mechanism of action</subject><subject>Mice</subject><subject>mortality</subject><subject>mosquito</subject><subject>mosquito control</subject><subject>Moths</subject><subject>Noctuidae</subject><subject>Plodia interpunctata</subject><subject>quinolines</subject><subject>Receptors, Steroid - agonists</subject><subject>Receptors, Steroid - genetics</subject><subject>Species Specificity</subject><subject>tetrahydroquinoline</subject><subject>toxicity</subject><subject>Transcriptional Activation</subject><issn>0739-4462</issn><issn>1520-6327</issn><fulltext>true</fulltext><rsrctype>article</rsrctype><creationdate>2005</creationdate><recordtype>article</recordtype><sourceid>EIF</sourceid><recordid>eNp9kU1P3DAQhi3UCraUCz-A5sShUqi_YjtHiFqohKjUFoG4WI4zZk2TGOxs6f77esm2vVUayaOZZ57Da4QOCT4hGNMPJtrlCcWYix20IBXFpWBUvkILLFldci7oHnqT0gPGuBZE7aI9UslKSIwX6OHMB7uEwVvTF0PooAiuMHbyYSzM2BWddw4ijJPP-838p5_WG2aE5wJst05hhMLch9GnKeXG-DFN2ZSeVn4KkF4sQ5iW6S167Uyf4GD77qPrTx-_Nxfl5Zfzz83pZWm5EqK0FWFG1kA70knmXCsoMEJa63LlhXLMOiWxqqu2Frx1pmqtqpQB5yh3jO2j49n7GMPTCtKkB58s9L0ZIaySJlJhSTjP4PsZtDGkFMHpx-gHE9eaYL1JVm-S1S_JZvhoa121A3T_0G2UGSAz8Ox7WP9HpU-_Nhd_pOV8k8ODX39vTPyhhWSy0jdX55re3t3e1M2VbjL_buadCdrcR5_09TeKCcs_W3NVU_YbbJOeeg</recordid><startdate>200504</startdate><enddate>200504</enddate><creator>Palli, S.R</creator><creator>Tice, C.M</creator><creator>Margam, V.M</creator><creator>Clark, A.M</creator><general>Wiley Subscription Services, Inc., A Wiley Company</general><scope>FBQ</scope><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>7SS</scope><scope>F1W</scope><scope>H95</scope><scope>L.G</scope></search><sort><creationdate>200504</creationdate><title>Biochemical mode of action and differential activity of new ecdysone agonists against mosquitoes and moths</title><author>Palli, S.R ; Tice, C.M ; Margam, V.M ; Clark, A.M</author></sort><facets><frbrtype>5</frbrtype><frbrgroupid>cdi_FETCH-LOGICAL-c4866-c513a79e2d1d73ffb62e311bcfbcfa798f3cf870895b964bfa5bc858aeff24f33</frbrgroupid><rsrctype>articles</rsrctype><prefilter>articles</prefilter><language>eng</language><creationdate>2005</creationdate><topic>3T3 Cells</topic><topic>Aedes</topic><topic>Aedes aegypti</topic><topic>Aminoquinolines - chemistry</topic><topic>Aminoquinolines - pharmacology</topic><topic>Animals</topic><topic>bioassays</topic><topic>Choristoneura fumiferana</topic><topic>Cloning, Molecular</topic><topic>Culicidae</topic><topic>diacylhydrazine</topic><topic>Drosophila melanogaster</topic><topic>ecdysone agonists</topic><topic>ecdysone receptor</topic><topic>ecdysone receptors</topic><topic>Heliothis</topic><topic>Heliothis virescens</topic><topic>hormone receptors</topic><topic>insecticidal properties</topic><topic>Insecticides - pharmacology</topic><topic>mechanism of action</topic><topic>Mice</topic><topic>mortality</topic><topic>mosquito</topic><topic>mosquito control</topic><topic>Moths</topic><topic>Noctuidae</topic><topic>Plodia interpunctata</topic><topic>quinolines</topic><topic>Receptors, Steroid - agonists</topic><topic>Receptors, Steroid - genetics</topic><topic>Species Specificity</topic><topic>tetrahydroquinoline</topic><topic>toxicity</topic><topic>Transcriptional Activation</topic><toplevel>peer_reviewed</toplevel><toplevel>online_resources</toplevel><creatorcontrib>Palli, S.R</creatorcontrib><creatorcontrib>Tice, C.M</creatorcontrib><creatorcontrib>Margam, V.M</creatorcontrib><creatorcontrib>Clark, A.M</creatorcontrib><collection>AGRIS</collection><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>Entomology Abstracts (Full archive)</collection><collection>ASFA: Aquatic Sciences and Fisheries Abstracts</collection><collection>Aquatic Science & Fisheries Abstracts (ASFA) 1: Biological Sciences & Living Resources</collection><collection>Aquatic Science & Fisheries Abstracts (ASFA) Professional</collection><jtitle>Archives of insect biochemistry and physiology</jtitle></facets><delivery><delcategory>Remote Search Resource</delcategory><fulltext>fulltext</fulltext></delivery><addata><au>Palli, S.R</au><au>Tice, C.M</au><au>Margam, V.M</au><au>Clark, A.M</au><format>journal</format><genre>article</genre><ristype>JOUR</ristype><atitle>Biochemical mode of action and differential activity of new ecdysone agonists against mosquitoes and moths</atitle><jtitle>Archives of insect biochemistry and physiology</jtitle><addtitle>Arch. Insect Biochem. Physiol</addtitle><date>2005-04</date><risdate>2005</risdate><volume>58</volume><issue>4</issue><spage>234</spage><epage>242</epage><pages>234-242</pages><issn>0739-4462</issn><eissn>1520-6327</eissn><abstract>THQ (1-aroyl-4-(arylamino)-1,2,3,4-tetrahydroquinoline) compounds were identified by FMC Corporation in cell-based assays that used ecdysone receptors from Drosophila melanogaster, Heliothis virescens, or Plodia interpunctata. THQ compounds showed weak insecticidal activity against H. virescens and, therefore, were not developed further. Several ecdysone agonists based on THQ chemotype have been synthesized and tested for their activity against a number of EcRs in transactivation assays. The THQ compound, RG-120768, activated AaEcR (EcR from A. aegypti) but did not activate EcRs cloned from other insects. In transactivation assays, all six THQ ligands tested functioned through AaEcR but not through CfEcR (EcR from Choristoneura fumiferana). Three THQ compounds that showed higher activity in transactivation assays were tested in tobacco bud moth, H. virescens, and yellow fever mosquito, A. aegypti. These compounds showed higher activity in A. aegypti when compared to their activity in H. virescens. These data show that the THQ ligands are a new class of non-steroidal ecdysone agonists with preferential activity against mosquitoes.</abstract><cop>Hoboken</cop><pub>Wiley Subscription Services, Inc., A Wiley Company</pub><pmid>15756700</pmid><doi>10.1002/arch.20046</doi><tpages>9</tpages></addata></record> |
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| subjects | 3T3 Cells Aedes Aedes aegypti Aminoquinolines - chemistry Aminoquinolines - pharmacology Animals bioassays Choristoneura fumiferana Cloning, Molecular Culicidae diacylhydrazine Drosophila melanogaster ecdysone agonists ecdysone receptor ecdysone receptors Heliothis Heliothis virescens hormone receptors insecticidal properties Insecticides - pharmacology mechanism of action Mice mortality mosquito mosquito control Moths Noctuidae Plodia interpunctata quinolines Receptors, Steroid - agonists Receptors, Steroid - genetics Species Specificity tetrahydroquinoline toxicity Transcriptional Activation |
| title | Biochemical mode of action and differential activity of new ecdysone agonists against mosquitoes and moths |
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