Screening and characterization of an inhibitory chemical specific to Arabidopsis gibberellin 2-oxidases
The hydroxylation of gibberellin (GA) at the 2-position is known as the major cause of inactivation of GAs, whose reaction is catalyzed by 2-oxoglutarate dependent dioxygenases, also termed GA 2-oxidases (GA2oxs). To block GA catabolism in plants, a few chemicals can be used. To obtain novel inhibit...
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Veröffentlicht in: | Bioorganic & medicinal chemistry letters 2010-07, Vol.20 (14), p.4259-4262 |
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creator | Otani, Masato Yoon, Jung-Min Park, Seung-Hyun Asami, Tadao Nakajima, Masatoshi |
description | The hydroxylation of gibberellin (GA) at the 2-position is known as the major cause of inactivation of GAs, whose reaction is catalyzed by 2-oxoglutarate dependent dioxygenases, also termed GA 2-oxidases (GA2oxs). To block GA catabolism in plants, a few chemicals can be used. To obtain novel inhibitors specific to GA2oxs, we performed in vitro random screenings by using 3H-16,17-dihydro-GA4 and recombinant Arabidopsis GA2ox2. As a result, one candidate, methyl 6-chloro-3H-1,2,3-benzodithiazole-4-carboxylate 2-oxide (CBTC), was selected from the screening, and was subjected to in-planta evaluations. CBTC promoted both the germination and elongation of Arabidopsis seedlings. This strongly suggests that CBTC inhibits GA2oxs in Arabidopsis with high specificity. |
doi_str_mv | 10.1016/j.bmcl.2010.05.015 |
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To block GA catabolism in plants, a few chemicals can be used. To obtain novel inhibitors specific to GA2oxs, we performed in vitro random screenings by using 3H-16,17-dihydro-GA4 and recombinant Arabidopsis GA2ox2. As a result, one candidate, methyl 6-chloro-3H-1,2,3-benzodithiazole-4-carboxylate 2-oxide (CBTC), was selected from the screening, and was subjected to in-planta evaluations. CBTC promoted both the germination and elongation of Arabidopsis seedlings. This strongly suggests that CBTC inhibits GA2oxs in Arabidopsis with high specificity.</description><identifier>ISSN: 0960-894X</identifier><identifier>EISSN: 1464-3405</identifier><identifier>DOI: 10.1016/j.bmcl.2010.05.015</identifier><identifier>PMID: 20570513</identifier><language>eng</language><publisher>Amsterdam: Elsevier Ltd</publisher><subject>2-Oxoglutarate dependent dioxygenase (2ODD) ; Agronomy. 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To block GA catabolism in plants, a few chemicals can be used. To obtain novel inhibitors specific to GA2oxs, we performed in vitro random screenings by using 3H-16,17-dihydro-GA4 and recombinant Arabidopsis GA2ox2. As a result, one candidate, methyl 6-chloro-3H-1,2,3-benzodithiazole-4-carboxylate 2-oxide (CBTC), was selected from the screening, and was subjected to in-planta evaluations. CBTC promoted both the germination and elongation of Arabidopsis seedlings. This strongly suggests that CBTC inhibits GA2oxs in Arabidopsis with high specificity.</description><subject>2-Oxoglutarate dependent dioxygenase (2ODD)</subject><subject>Agronomy. Soil science and plant productions</subject><subject>Arabidopsis</subject><subject>Arabidopsis - enzymology</subject><subject>Arabidopsis - growth & development</subject><subject>Biological and medical sciences</subject><subject>Economic plant physiology</subject><subject>Fundamental and applied biological sciences. Psychology</subject><subject>Gibberellin</subject><subject>Gibberellin 2-oxidase</subject><subject>Growth and development</subject><subject>Growth regulators</subject><subject>Inhibitor</subject><subject>Mixed Function Oxygenases - metabolism</subject><issn>0960-894X</issn><issn>1464-3405</issn><fulltext>true</fulltext><rsrctype>article</rsrctype><creationdate>2010</creationdate><recordtype>article</recordtype><sourceid>EIF</sourceid><recordid>eNqFkU-LFDEQxYMo7rj6BTxIX8RTj0mn0t0DXpbFf7DgQQVvIalUz9bQ3RmTnsX105thRr3pqaD4vcfjPSGeK7lWUrWvd2s_4bhuZHlIs5bKPBArBS3UGqR5KFZy08q638C3C_Ek552UCiTAY3HRSNNJo_RKbD9jIpp53lZuDhXeuuRwocQ_3cJxruJQ_hXPt-x5iem-EDQxurHKe0IeGKslVlfJeQ5xnzlXW_aeEo0jz1VTxx8cXKb8VDwa3Jjp2fleiq_v3n65_lDffHr_8frqpkbo9VIH0wTSKrTkIfjNQB1I71sE5YCc2gT03mnfgDJGYicHr9pO6d6Ddx471Jfi1cl3n-L3A-XFTpyxpHEzxUO2nQEDsm_g_6TWrWn6VheyOZGYYs6JBrtPPLl0b5W0xyXszh6XsMclrDS2LFFEL872Bz9R-CP5XX0BXp4Bl0ufQ3Izcv7L6WIGcMz55sRRqe2OKdmMTDNS4ES42BD5Xzl-AQd0qJ4</recordid><startdate>20100715</startdate><enddate>20100715</enddate><creator>Otani, Masato</creator><creator>Yoon, Jung-Min</creator><creator>Park, Seung-Hyun</creator><creator>Asami, Tadao</creator><creator>Nakajima, Masatoshi</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>7X8</scope><scope>7QO</scope><scope>8FD</scope><scope>FR3</scope><scope>P64</scope></search><sort><creationdate>20100715</creationdate><title>Screening and characterization of an inhibitory chemical specific to Arabidopsis gibberellin 2-oxidases</title><author>Otani, Masato ; Yoon, Jung-Min ; Park, Seung-Hyun ; Asami, Tadao ; Nakajima, Masatoshi</author></sort><facets><frbrtype>5</frbrtype><frbrgroupid>cdi_FETCH-LOGICAL-c483t-d52de31d6eb4db9fe740bb6c41a4ea19dcbba3b241550c70fb167138b4babc7c3</frbrgroupid><rsrctype>articles</rsrctype><prefilter>articles</prefilter><language>eng</language><creationdate>2010</creationdate><topic>2-Oxoglutarate dependent dioxygenase (2ODD)</topic><topic>Agronomy. Soil science and plant productions</topic><topic>Arabidopsis</topic><topic>Arabidopsis - enzymology</topic><topic>Arabidopsis - growth & development</topic><topic>Biological and medical sciences</topic><topic>Economic plant physiology</topic><topic>Fundamental and applied biological sciences. Psychology</topic><topic>Gibberellin</topic><topic>Gibberellin 2-oxidase</topic><topic>Growth and development</topic><topic>Growth regulators</topic><topic>Inhibitor</topic><topic>Mixed Function Oxygenases - metabolism</topic><toplevel>peer_reviewed</toplevel><toplevel>online_resources</toplevel><creatorcontrib>Otani, Masato</creatorcontrib><creatorcontrib>Yoon, Jung-Min</creatorcontrib><creatorcontrib>Park, Seung-Hyun</creatorcontrib><creatorcontrib>Asami, Tadao</creatorcontrib><creatorcontrib>Nakajima, Masatoshi</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>MEDLINE - Academic</collection><collection>Biotechnology Research Abstracts</collection><collection>Technology Research Database</collection><collection>Engineering Research Database</collection><collection>Biotechnology and BioEngineering Abstracts</collection><jtitle>Bioorganic & medicinal chemistry letters</jtitle></facets><delivery><delcategory>Remote Search Resource</delcategory><fulltext>fulltext</fulltext></delivery><addata><au>Otani, Masato</au><au>Yoon, Jung-Min</au><au>Park, Seung-Hyun</au><au>Asami, Tadao</au><au>Nakajima, Masatoshi</au><format>journal</format><genre>article</genre><ristype>JOUR</ristype><atitle>Screening and characterization of an inhibitory chemical specific to Arabidopsis gibberellin 2-oxidases</atitle><jtitle>Bioorganic & medicinal chemistry letters</jtitle><addtitle>Bioorg Med Chem Lett</addtitle><date>2010-07-15</date><risdate>2010</risdate><volume>20</volume><issue>14</issue><spage>4259</spage><epage>4262</epage><pages>4259-4262</pages><issn>0960-894X</issn><eissn>1464-3405</eissn><abstract>The hydroxylation of gibberellin (GA) at the 2-position is known as the major cause of inactivation of GAs, whose reaction is catalyzed by 2-oxoglutarate dependent dioxygenases, also termed GA 2-oxidases (GA2oxs). 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subjects | 2-Oxoglutarate dependent dioxygenase (2ODD) Agronomy. Soil science and plant productions Arabidopsis Arabidopsis - enzymology Arabidopsis - growth & development Biological and medical sciences Economic plant physiology Fundamental and applied biological sciences. Psychology Gibberellin Gibberellin 2-oxidase Growth and development Growth regulators Inhibitor Mixed Function Oxygenases - metabolism |
title | Screening and characterization of an inhibitory chemical specific to Arabidopsis gibberellin 2-oxidases |
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