Journal Article

The Phenylquinazoline Compound S-4893 is a Non-Competitive Cytokinin Antagonist that Targets Arabidopsis Cytokinin Receptor CRE1 and Promotes Root Growth in Arabidopsis and Rice

Yuto Arata, Asako Nagasawa-Iida, Hideki Uneme, Hiroki Nakajima, Tatsuo Kakimoto and Ryo Sato

in Plant and Cell Physiology

Published on behalf of Japanese Society of Plant Physiologists

Volume 51, issue 12, pages 2047-2059
Published in print December 2010 | ISSN: 0032-0781
Published online November 2010 | e-ISSN: 1471-9053 | DOI: http://dx.doi.org/10.1093/pcp/pcq163
The Phenylquinazoline Compound S-4893 is a Non-Competitive Cytokinin Antagonist that Targets Arabidopsis Cytokinin Receptor CRE1 and Promotes Root Growth in Arabidopsis and Rice

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We identified two phenylquinazoline compounds in a large-scale screening for cytokinin antagonists in yeast expressing the Arabidopsis cytokinin receptor cytokinin response 1/histidine kinase 4 (CRE1). After chemical modifications, we obtained compound S-4893, which non-competitively inhibited binding of the natural ligand 2-isopentenyladenine to CRE1. S-4893 antagonized cytokinin-induced activation of the Arabidopsis response regulator 5 promoter in Arabidopsis. Importantly, S-4893 had no detectable intrinsic cytokinin agonist activity in Arabidopsis or in the transformed yeast system. Cytokinin bioassay further demonstrated that S-4893 antagonized cytokinin-induced stimulation of callus formation and inhibition of root elongation. S-4893 also promoted seminal, crown and lateral root growth in rice, suggesting that S-4893 could potentially promote root growth in a variety of agronomically important plants. We believe S-4893 will be a useful tool in functional studies of cytokinin action in a wide range of plants and a lead compound for the development of useful root growth promoters in agriculture.

Keywords: Arabidopsis thaliana; Cytokinin; Cytokinin antagonist; Cytokinin receptor; Plant growth regulator; Root growth promoter

Journal Article.  7384 words.  Illustrated.

Subjects: Biochemistry ; Molecular and Cell Biology ; Plant Sciences and Forestry

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