Identification of novel juvenile-hormone signaling activators via high-throughput screening with a chemical library
Juvenile hormone (JH) is an insect-specific hormone that regulates molting and metamorphosis. Hence, JH signaling inhibitors (JHSIs) and activators (JHSAs) can be used as effective insect growth regulators (IGRs) for pest management. In our previous study, we established a high-throughput screening...
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| Veröffentlicht in: | Journal of Pesticide Science 2021/02/20, Vol.46(1), pp.53-59 |
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| creator | Kayukawa, Takumi Furuta, Kenjiro Yonesu, Kiyoaki Okabe, Takayoshi |
| description | Juvenile hormone (JH) is an insect-specific hormone that regulates molting and metamorphosis. Hence, JH signaling inhibitors (JHSIs) and activators (JHSAs) can be used as effective insect growth regulators (IGRs) for pest management. In our previous study, we established a high-throughput screening (HTS) system for exploration of novel JHSIs and JHSAs using a Bombyx mori cell line (BmN_JF&AR cells) and succeeded in identifying novel JHSIs from a chemical library. Here, we searched for novel JHSAs using this system. The four-step HTS yielded 10 compounds as candidate JHSAs; some of these compounds showed novel basic structures, whereas the others were composed of a 4-phenoxyphenoxymethyl skeleton, the basic structure of several existing JH analogs (pyriproxyfen and fenoxycarb). Topical application of seven compounds to B. mori larvae significantly prolonged the larval period, suggesting that the identified JHSAs may be promising IGRs targeting the JH signaling pathway. |
| doi_str_mv | 10.1584/jpestics.D20-070 |
| format | Article |
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Hence, JH signaling inhibitors (JHSIs) and activators (JHSAs) can be used as effective insect growth regulators (IGRs) for pest management. In our previous study, we established a high-throughput screening (HTS) system for exploration of novel JHSIs and JHSAs using a Bombyx mori cell line (BmN_JF&AR cells) and succeeded in identifying novel JHSIs from a chemical library. Here, we searched for novel JHSAs using this system. The four-step HTS yielded 10 compounds as candidate JHSAs; some of these compounds showed novel basic structures, whereas the others were composed of a 4-phenoxyphenoxymethyl skeleton, the basic structure of several existing JH analogs (pyriproxyfen and fenoxycarb). 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This is an open access article distributed under the Creative Commons Attribution-NonCommercial-NoDerivatives 4.0 International (CC BY-NC-ND 4.0) License (https://creativecommons.org/licenses/by-nc-nd/4.0/) International (CC BY-NC-ND 4.0) License (https://creativecommons.org/licenses/by-nc-nd/4.0/)</rights><lds50>peer_reviewed</lds50><oa>free_for_read</oa><woscitedreferencessubscribed>false</woscitedreferencessubscribed><citedby>FETCH-LOGICAL-c553t-f6d894b7933c59726158876b36ca9bf7a41c4775a22701e6919bc99d68017efe3</citedby><cites>FETCH-LOGICAL-c553t-f6d894b7933c59726158876b36ca9bf7a41c4775a22701e6919bc99d68017efe3</cites></display><links><openurl>$$Topenurl_article</openurl><openurlfulltext>$$Topenurlfull_article</openurlfulltext><thumbnail>$$Tsyndetics_thumb_exl</thumbnail><linktopdf>$$Uhttps://www.ncbi.nlm.nih.gov/pmc/articles/PMC7953030/pdf/$$EPDF$$P50$$Gpubmedcentral$$H</linktopdf><linktohtml>$$Uhttps://www.ncbi.nlm.nih.gov/pmc/articles/PMC7953030/$$EHTML$$P50$$Gpubmedcentral$$H</linktohtml><link.rule.ids>230,314,723,776,780,860,881,1877,27901,27902,53766,53768</link.rule.ids><backlink>$$Uhttps://www.ncbi.nlm.nih.gov/pubmed/33746546$$D View this record in MEDLINE/PubMed$$Hfree_for_read</backlink></links><search><creatorcontrib>Kayukawa, Takumi</creatorcontrib><creatorcontrib>Furuta, Kenjiro</creatorcontrib><creatorcontrib>Yonesu, Kiyoaki</creatorcontrib><creatorcontrib>Okabe, Takayoshi</creatorcontrib><title>Identification of novel juvenile-hormone signaling activators via high-throughput screening with a chemical library</title><title>Journal of Pesticide Science</title><addtitle>J. Pestic. Sci.</addtitle><description>Juvenile hormone (JH) is an insect-specific hormone that regulates molting and metamorphosis. Hence, JH signaling inhibitors (JHSIs) and activators (JHSAs) can be used as effective insect growth regulators (IGRs) for pest management. In our previous study, we established a high-throughput screening (HTS) system for exploration of novel JHSIs and JHSAs using a Bombyx mori cell line (BmN_JF&AR cells) and succeeded in identifying novel JHSIs from a chemical library. Here, we searched for novel JHSAs using this system. The four-step HTS yielded 10 compounds as candidate JHSAs; some of these compounds showed novel basic structures, whereas the others were composed of a 4-phenoxyphenoxymethyl skeleton, the basic structure of several existing JH analogs (pyriproxyfen and fenoxycarb). Topical application of seven compounds to B. mori larvae significantly prolonged the larval period, suggesting that the identified JHSAs may be promising IGRs targeting the JH signaling pathway.</description><subject>Bombyx mori</subject><subject>Fenoxycarb</subject><subject>Growth regulators</subject><subject>High-throughput screening</subject><subject>insect growth regulator</subject><subject>Insecticides</subject><subject>Insects</subject><subject>juvenile hormone</subject><subject>juvenile hormone signaling activator</subject><subject>Juvenile hormones</subject><subject>Larvae</subject><subject>Libraries</subject><subject>Metamorphosis</subject><subject>Molting</subject><subject>Pest control</subject><subject>pest management</subject><subject>Pyriproxyfen</subject><subject>Regular</subject><subject>Screening</subject><subject>Signal transduction</subject><subject>Signaling</subject><subject>Topical application</subject><issn>1348-589X</issn><issn>1349-0923</issn><fulltext>true</fulltext><rsrctype>article</rsrctype><creationdate>2021</creationdate><recordtype>article</recordtype><recordid>eNpdkc1rFTEUxYMotjy7dyUBN26mJpOvyUaQamuh4EbBXcjkZWYyZJJnknnF_9607_X5QSC5kN893HMPAK8xusSso-_nnc3FmXz5qUUNEugZOMeEygbJljx_rLuGdfLHGbjIeUYIYUGElPwlOCNEUM4oPwf5dmtDcYMzurgYYBxgiHvr4bzubXDeNlNMSwwWZjcG7V0YoTbF7XWJKcO903By49SUKcV1nHZrgdkkW1sreO_KBDU0k12qvofe9UmnX6_Ai0H7bC-O7wZ8v_787epLc_f15vbq411jGCOlGfi2k7QXkhDDpGh5dd0J3hNutOwHoSk2VAim21YgbLnEsjdSbnlXndrBkg34cNDdrf1it6YaTdqrXXJLnUJF7dS_P8FNaox7JSQjqJ4NeHcUSPHnWretFpeN9V4HG9esWoYI55xiVtG3_6FzXFNdWKWopJJJinml0IEyKeac7HAaBiP1EKp6ClXVUFUNtba8-dvEqeEpwgpcH4A5Fz3aE6BT1fH2jyLlCj9cR-UTYCadlA3kNwyFu9A</recordid><startdate>20210220</startdate><enddate>20210220</enddate><creator>Kayukawa, Takumi</creator><creator>Furuta, Kenjiro</creator><creator>Yonesu, Kiyoaki</creator><creator>Okabe, Takayoshi</creator><general>Pesticide Science Society of Japan</general><general>Japan Science and Technology Agency</general><scope>NPM</scope><scope>AAYXX</scope><scope>CITATION</scope><scope>7SS</scope><scope>7ST</scope><scope>7TK</scope><scope>7U7</scope><scope>C1K</scope><scope>SOI</scope><scope>7X8</scope><scope>5PM</scope></search><sort><creationdate>20210220</creationdate><title>Identification of novel juvenile-hormone signaling activators via high-throughput screening with a chemical library</title><author>Kayukawa, Takumi ; Furuta, Kenjiro ; Yonesu, Kiyoaki ; Okabe, Takayoshi</author></sort><facets><frbrtype>5</frbrtype><frbrgroupid>cdi_FETCH-LOGICAL-c553t-f6d894b7933c59726158876b36ca9bf7a41c4775a22701e6919bc99d68017efe3</frbrgroupid><rsrctype>articles</rsrctype><prefilter>articles</prefilter><language>eng</language><creationdate>2021</creationdate><topic>Bombyx mori</topic><topic>Fenoxycarb</topic><topic>Growth regulators</topic><topic>High-throughput screening</topic><topic>insect growth regulator</topic><topic>Insecticides</topic><topic>Insects</topic><topic>juvenile hormone</topic><topic>juvenile hormone signaling activator</topic><topic>Juvenile hormones</topic><topic>Larvae</topic><topic>Libraries</topic><topic>Metamorphosis</topic><topic>Molting</topic><topic>Pest control</topic><topic>pest management</topic><topic>Pyriproxyfen</topic><topic>Regular</topic><topic>Screening</topic><topic>Signal transduction</topic><topic>Signaling</topic><topic>Topical application</topic><toplevel>peer_reviewed</toplevel><toplevel>online_resources</toplevel><creatorcontrib>Kayukawa, Takumi</creatorcontrib><creatorcontrib>Furuta, Kenjiro</creatorcontrib><creatorcontrib>Yonesu, Kiyoaki</creatorcontrib><creatorcontrib>Okabe, Takayoshi</creatorcontrib><collection>PubMed</collection><collection>CrossRef</collection><collection>Entomology Abstracts (Full archive)</collection><collection>Environment Abstracts</collection><collection>Neurosciences Abstracts</collection><collection>Toxicology Abstracts</collection><collection>Environmental Sciences and Pollution Management</collection><collection>Environment Abstracts</collection><collection>MEDLINE - Academic</collection><collection>PubMed Central (Full Participant titles)</collection><jtitle>Journal of Pesticide Science</jtitle></facets><delivery><delcategory>Remote Search Resource</delcategory><fulltext>fulltext</fulltext></delivery><addata><au>Kayukawa, Takumi</au><au>Furuta, Kenjiro</au><au>Yonesu, Kiyoaki</au><au>Okabe, Takayoshi</au><format>journal</format><genre>article</genre><ristype>JOUR</ristype><atitle>Identification of novel juvenile-hormone signaling activators via high-throughput screening with a chemical library</atitle><jtitle>Journal of Pesticide Science</jtitle><addtitle>J. Pestic. Sci.</addtitle><date>2021-02-20</date><risdate>2021</risdate><volume>46</volume><issue>1</issue><spage>53</spage><epage>59</epage><pages>53-59</pages><issn>1348-589X</issn><eissn>1349-0923</eissn><abstract>Juvenile hormone (JH) is an insect-specific hormone that regulates molting and metamorphosis. Hence, JH signaling inhibitors (JHSIs) and activators (JHSAs) can be used as effective insect growth regulators (IGRs) for pest management. In our previous study, we established a high-throughput screening (HTS) system for exploration of novel JHSIs and JHSAs using a Bombyx mori cell line (BmN_JF&AR cells) and succeeded in identifying novel JHSIs from a chemical library. Here, we searched for novel JHSAs using this system. The four-step HTS yielded 10 compounds as candidate JHSAs; some of these compounds showed novel basic structures, whereas the others were composed of a 4-phenoxyphenoxymethyl skeleton, the basic structure of several existing JH analogs (pyriproxyfen and fenoxycarb). Topical application of seven compounds to B. mori larvae significantly prolonged the larval period, suggesting that the identified JHSAs may be promising IGRs targeting the JH signaling pathway.</abstract><cop>Japan</cop><pub>Pesticide Science Society of Japan</pub><pmid>33746546</pmid><doi>10.1584/jpestics.D20-070</doi><tpages>7</tpages><oa>free_for_read</oa></addata></record> |
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| subjects | Bombyx mori Fenoxycarb Growth regulators High-throughput screening insect growth regulator Insecticides Insects juvenile hormone juvenile hormone signaling activator Juvenile hormones Larvae Libraries Metamorphosis Molting Pest control pest management Pyriproxyfen Regular Screening Signal transduction Signaling Topical application |
| title | Identification of novel juvenile-hormone signaling activators via high-throughput screening with a chemical library |
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