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Activation of mammalian retinoid X receptors by the insect growth regulator methoprene
We report that methoprene and its derivatives can stimulate gene transcription in vertebrates by acting through the retinoic acid-responsive transcription factors, the retinoid X receptors (RXRs). Methoprene is an insect growth regulator in domestic and agricultural use as a pesticide. At least one...
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| Published in: | Proceedings of the National Academy of Sciences - PNAS 1995-06, Vol.92 (13), p.6157-6160 |
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| Main Authors: | , , , |
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| container_end_page | 6160 |
| container_issue | 13 |
| container_start_page | 6157 |
| container_title | Proceedings of the National Academy of Sciences - PNAS |
| container_volume | 92 |
| creator | Harmon, M A Boehm, M F Heyman, R A Mangelsdorf, D J |
| description | We report that methoprene and its derivatives can stimulate gene transcription in vertebrates by acting through the retinoic acid-responsive transcription factors, the retinoid X receptors (RXRs). Methoprene is an insect growth regulator in domestic and agricultural use as a pesticide. At least one metabolite of methoprene, methoprene acid, directly binds to RXR and is a transcriptional activator in both insect and mammalian cells. Unlike the endogenous RXR ligand, 9-cis-retinoic acid, this activity is RXR-specific; the methoprene derivatives do not activate the retinoic acid receptor pathway. Methoprene is a juvenile hormone analog that acts to retain juvenile characteristics during insect growth, preventing metamorphosis into an adult, and it has been shown to have ovicidal properties in some insects. Thus, a pesticide that mimics the action of juvenile hormone in insects can also activate a mammalian retinoid-responsive pathway. This finding provides a basis through which the potential bioactivity of substances exposed to the environment may be reexamined and points the way for discovery of new receptor ligands in both insects and vertebrates. |
| doi_str_mv | 10.1073/pnas.92.13.6157 |
| format | article |
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Methoprene is an insect growth regulator in domestic and agricultural use as a pesticide. At least one metabolite of methoprene, methoprene acid, directly binds to RXR and is a transcriptional activator in both insect and mammalian cells. Unlike the endogenous RXR ligand, 9-cis-retinoic acid, this activity is RXR-specific; the methoprene derivatives do not activate the retinoic acid receptor pathway. Methoprene is a juvenile hormone analog that acts to retain juvenile characteristics during insect growth, preventing metamorphosis into an adult, and it has been shown to have ovicidal properties in some insects. Thus, a pesticide that mimics the action of juvenile hormone in insects can also activate a mammalian retinoid-responsive pathway. 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Methoprene is an insect growth regulator in domestic and agricultural use as a pesticide. At least one metabolite of methoprene, methoprene acid, directly binds to RXR and is a transcriptional activator in both insect and mammalian cells. Unlike the endogenous RXR ligand, 9-cis-retinoic acid, this activity is RXR-specific; the methoprene derivatives do not activate the retinoic acid receptor pathway. Methoprene is a juvenile hormone analog that acts to retain juvenile characteristics during insect growth, preventing metamorphosis into an adult, and it has been shown to have ovicidal properties in some insects. Thus, a pesticide that mimics the action of juvenile hormone in insects can also activate a mammalian retinoid-responsive pathway. This finding provides a basis through which the potential bioactivity of substances exposed to the environment may be reexamined and points the way for discovery of new receptor ligands in both insects and vertebrates.</description><subject>Animals</subject><subject>beta-Galactosidase - biosynthesis</subject><subject>Binding, Competitive</subject><subject>Biochemistry</subject><subject>Cell Line</subject><subject>Cercopithecus aethiops</subject><subject>DNA-Binding Proteins</subject><subject>Drosophila</subject><subject>Drosophila melanogaster</subject><subject>Fungal Proteins - biosynthesis</subject><subject>Fungal Proteins - metabolism</subject><subject>Gene Expression - drug effects</subject><subject>Genes</subject><subject>Insects</subject><subject>Kidney</subject><subject>Kinetics</subject><subject>Luciferases - biosynthesis</subject><subject>Luciferases - metabolism</subject><subject>Methoprene - pharmacology</subject><subject>Receptors, Retinoic Acid - biosynthesis</subject><subject>Receptors, Retinoic Acid - drug effects</subject><subject>Receptors, Retinoic Acid - metabolism</subject><subject>Recombinant Proteins - biosynthesis</subject><subject>Recombinant Proteins - drug effects</subject><subject>Recombinant Proteins - metabolism</subject><subject>Retinoid X Receptors</subject><subject>Retinoids - metabolism</subject><subject>Saccharomyces cerevisiae Proteins</subject><subject>Transcription Factors - biosynthesis</subject><subject>Transcription Factors - drug effects</subject><subject>Transcription Factors - metabolism</subject><subject>Transcription, Genetic - drug effects</subject><subject>Transfection</subject><subject>Vertebrates</subject><issn>0027-8424</issn><issn>1091-6490</issn><fulltext>true</fulltext><rsrctype>article</rsrctype><creationdate>1995</creationdate><recordtype>article</recordtype><recordid>eNqFkU1vFSEUhomxqdfq2pVm4kJXc3tg-Lgk3TSNX0mTbtS4I0CZe2lmYASm2n8vk16rdmFXkDzPe8LhRegFhjUG0R1PQee1JGvcrTlm4hFaYZC45VTCY7QCIKLdUEKfoKc5XwGAZBs4RIeCSQGSr9DXU1v8tS4-hib2zajHUQ9ehya54kP0l823erVuKjHlxtw0ZecaH7Kzpdmm-KPsKt7Og668GV3ZxSm54J6hg14P2T3fn0foy_t3n88-tucXHz6dnZ63lnFWWswcEc5Y3QugXBsDwHWPnQUpCbHSCCk0NwJTyiiT2gAhTPTWakqNoF13hE5u506zGd2ldaEkPagp-VGnGxW1V_-S4HdqG68VxZzjGn-zj6f4fXa5qNFn64ZBBxfnrITohCCMPihivukw3izi63viVZxTqH-gCGAisSRQpeNbyaaYc3L93YMxqKVWtdSqJFG4U0utNfHy7z3v_H2Plb_d8yX4m_4ZoPp5GIr7War56r9m9wsWubfk</recordid><startdate>19950620</startdate><enddate>19950620</enddate><creator>Harmon, M A</creator><creator>Boehm, M F</creator><creator>Heyman, R A</creator><creator>Mangelsdorf, D J</creator><general>National Acad Sciences</general><general>National Academy of Sciences</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>7QG</scope><scope>7QL</scope><scope>7QP</scope><scope>7QR</scope><scope>7SN</scope><scope>7SS</scope><scope>7T5</scope><scope>7TK</scope><scope>7TM</scope><scope>7TO</scope><scope>7U9</scope><scope>8FD</scope><scope>C1K</scope><scope>FR3</scope><scope>H94</scope><scope>M7N</scope><scope>P64</scope><scope>RC3</scope><scope>7X8</scope><scope>5PM</scope></search><sort><creationdate>19950620</creationdate><title>Activation of mammalian retinoid X receptors by the insect growth regulator methoprene</title><author>Harmon, M A ; Boehm, M F ; Heyman, R A ; Mangelsdorf, D J</author></sort><facets><frbrtype>5</frbrtype><frbrgroupid>cdi_FETCH-LOGICAL-c565t-15e27ebcaf7046abb006af1ec09922c9b797a6b71445459ab02257fcca44b7433</frbrgroupid><rsrctype>articles</rsrctype><prefilter>articles</prefilter><language>eng</language><creationdate>1995</creationdate><topic>Animals</topic><topic>beta-Galactosidase - biosynthesis</topic><topic>Binding, Competitive</topic><topic>Biochemistry</topic><topic>Cell Line</topic><topic>Cercopithecus aethiops</topic><topic>DNA-Binding Proteins</topic><topic>Drosophila</topic><topic>Drosophila melanogaster</topic><topic>Fungal Proteins - biosynthesis</topic><topic>Fungal Proteins - metabolism</topic><topic>Gene Expression - drug effects</topic><topic>Genes</topic><topic>Insects</topic><topic>Kidney</topic><topic>Kinetics</topic><topic>Luciferases - biosynthesis</topic><topic>Luciferases - metabolism</topic><topic>Methoprene - pharmacology</topic><topic>Receptors, Retinoic Acid - biosynthesis</topic><topic>Receptors, Retinoic Acid - drug effects</topic><topic>Receptors, Retinoic Acid - metabolism</topic><topic>Recombinant Proteins - biosynthesis</topic><topic>Recombinant Proteins - drug effects</topic><topic>Recombinant Proteins - metabolism</topic><topic>Retinoid X Receptors</topic><topic>Retinoids - metabolism</topic><topic>Saccharomyces cerevisiae Proteins</topic><topic>Transcription Factors - biosynthesis</topic><topic>Transcription Factors - drug effects</topic><topic>Transcription Factors - metabolism</topic><topic>Transcription, Genetic - drug effects</topic><topic>Transfection</topic><topic>Vertebrates</topic><toplevel>peer_reviewed</toplevel><toplevel>online_resources</toplevel><creatorcontrib>Harmon, M A</creatorcontrib><creatorcontrib>Boehm, M F</creatorcontrib><creatorcontrib>Heyman, R A</creatorcontrib><creatorcontrib>Mangelsdorf, D J</creatorcontrib><collection>Medline</collection><collection>MEDLINE</collection><collection>MEDLINE (Ovid)</collection><collection>MEDLINE</collection><collection>MEDLINE</collection><collection>PubMed</collection><collection>CrossRef</collection><collection>Animal Behavior Abstracts</collection><collection>Bacteriology Abstracts (Microbiology B)</collection><collection>Calcium & Calcified Tissue Abstracts</collection><collection>Chemoreception Abstracts</collection><collection>Ecology Abstracts</collection><collection>Entomology Abstracts (Full archive)</collection><collection>Immunology Abstracts</collection><collection>Neurosciences Abstracts</collection><collection>Nucleic Acids Abstracts</collection><collection>Oncogenes and Growth Factors Abstracts</collection><collection>Virology and AIDS Abstracts</collection><collection>Technology Research Database</collection><collection>Environmental Sciences and Pollution Management</collection><collection>Engineering Research Database</collection><collection>AIDS and Cancer Research Abstracts</collection><collection>Algology Mycology and Protozoology Abstracts (Microbiology C)</collection><collection>Biotechnology and BioEngineering Abstracts</collection><collection>Genetics Abstracts</collection><collection>MEDLINE - Academic</collection><collection>PubMed Central (Full Participant titles)</collection><jtitle>Proceedings of the National Academy of Sciences - PNAS</jtitle></facets><delivery><delcategory>Remote Search Resource</delcategory><fulltext>fulltext</fulltext></delivery><addata><au>Harmon, M A</au><au>Boehm, M F</au><au>Heyman, R A</au><au>Mangelsdorf, D J</au><format>journal</format><genre>article</genre><ristype>JOUR</ristype><atitle>Activation of mammalian retinoid X receptors by the insect growth regulator methoprene</atitle><jtitle>Proceedings of the National Academy of Sciences - PNAS</jtitle><addtitle>Proc Natl Acad Sci U S A</addtitle><date>1995-06-20</date><risdate>1995</risdate><volume>92</volume><issue>13</issue><spage>6157</spage><epage>6160</epage><pages>6157-6160</pages><issn>0027-8424</issn><eissn>1091-6490</eissn><notes>ObjectType-Article-2</notes><notes>SourceType-Scholarly Journals-1</notes><notes>ObjectType-Feature-1</notes><notes>content type line 23</notes><notes>ObjectType-Article-1</notes><notes>ObjectType-Feature-2</notes><abstract>We report that methoprene and its derivatives can stimulate gene transcription in vertebrates by acting through the retinoic acid-responsive transcription factors, the retinoid X receptors (RXRs). Methoprene is an insect growth regulator in domestic and agricultural use as a pesticide. At least one metabolite of methoprene, methoprene acid, directly binds to RXR and is a transcriptional activator in both insect and mammalian cells. Unlike the endogenous RXR ligand, 9-cis-retinoic acid, this activity is RXR-specific; the methoprene derivatives do not activate the retinoic acid receptor pathway. Methoprene is a juvenile hormone analog that acts to retain juvenile characteristics during insect growth, preventing metamorphosis into an adult, and it has been shown to have ovicidal properties in some insects. Thus, a pesticide that mimics the action of juvenile hormone in insects can also activate a mammalian retinoid-responsive pathway. This finding provides a basis through which the potential bioactivity of substances exposed to the environment may be reexamined and points the way for discovery of new receptor ligands in both insects and vertebrates.</abstract><cop>United States</cop><pub>National Acad Sciences</pub><pmid>7597096</pmid><doi>10.1073/pnas.92.13.6157</doi><tpages>4</tpages><oa>free_for_read</oa></addata></record> |
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| identifier | ISSN: 0027-8424 |
| ispartof | Proceedings of the National Academy of Sciences - PNAS, 1995-06, Vol.92 (13), p.6157-6160 |
| issn | 0027-8424 1091-6490 |
| language | eng |
| recordid | cdi_proquest_journals_201291920 |
| source | JSTOR Archival Journals and Primary Sources Collection; PubMed Central |
| subjects | Animals beta-Galactosidase - biosynthesis Binding, Competitive Biochemistry Cell Line Cercopithecus aethiops DNA-Binding Proteins Drosophila Drosophila melanogaster Fungal Proteins - biosynthesis Fungal Proteins - metabolism Gene Expression - drug effects Genes Insects Kidney Kinetics Luciferases - biosynthesis Luciferases - metabolism Methoprene - pharmacology Receptors, Retinoic Acid - biosynthesis Receptors, Retinoic Acid - drug effects Receptors, Retinoic Acid - metabolism Recombinant Proteins - biosynthesis Recombinant Proteins - drug effects Recombinant Proteins - metabolism Retinoid X Receptors Retinoids - metabolism Saccharomyces cerevisiae Proteins Transcription Factors - biosynthesis Transcription Factors - drug effects Transcription Factors - metabolism Transcription, Genetic - drug effects Transfection Vertebrates |
| title | Activation of mammalian retinoid X receptors by the insect growth regulator methoprene |
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