Screening and characterization of an inhibitory chemical specific to Arabidopsis gibberellin 2-oxidases

Bioorg Med Chem Lett. 2010 Jul 15;20(14):4259-62. doi: 10.1016/j.bmcl.2010.05.015. Epub 2010 May 19.

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). 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 (3)H-16,17-dihydro-GA(4) 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.

Publication types

  • Research Support, Non-U.S. Gov't

MeSH terms

  • Arabidopsis / enzymology*
  • Arabidopsis / growth & development
  • Mixed Function Oxygenases / metabolism*

Substances

  • Mixed Function Oxygenases
  • gibberellin 2-dioxygenase