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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Bibliographic Details
Published in:Bioorganic & medicinal chemistry letters 2010-07, Vol.20 (14), p.4259-4262
Main Authors: Otani, Masato, Yoon, Jung-Min, Park, Seung-Hyun, Asami, Tadao, Nakajima, Masatoshi
Format: Article
Language:English
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
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Summary: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.
ISSN:0960-894X
1464-3405
DOI:10.1016/j.bmcl.2010.05.015