The aim of this study was to investigate the action spectrum of two urea derivatives, the 1,3-di(benzo[d]oxazol-5-yl)urea (5-BDPU) and the 1,3-di(benzo[d]oxazol-6-yl)urea (6-BDPU). In order to evaluate a possible adjuvant activity on cytokinins the compounds alone or in the simultaneous presence of different cytokinins were assayed either on in vitro typical cytokinin-related bioassays, or on in planta interaction with cytokinin signal transduction pathway. The compounds ability to activate the cytokinin receptor CRE1/AHK4 was studied either by a heterologous bacterial assay or by a competitive binding assay and docking simulations were performed with the crystal structure of the same receptor. Then, owing to their chemical structure which resembles that of urea-type cytokinins, the ability of 5- and 6-BDPU to inhibit the activity of cytokinin oxidase/dehydrogenase of Zea mays (ZmCKX1) was investigated and docking simulations were performed as well. Accordingly to the experimental results, we speculate that BDPUs could show a dual activity: the blocking of the conformational re-adaption of CRE1/AHK4 receptor maintaining the cytokinin inside its binding pocket, thus possibly enhancing its kinase action; the inhibition of cytokinin oxidase/dehydrogenase activity thus possibly preventing its cleavage of natural cytokinins with isoprenoid side chain. Graphic abstract: [Figure not available: see fulltext.]

The adjuvant activity of two urea derivatives on cytokinins: an example of serendipitous dual effect / Brunoni, F.; Rolli, E.; Polverini, E.; Spichal, L.; Ricci, A.. - In: PLANT GROWTH REGULATION. - ISSN 0167-6903. - 95:(2021), pp. 169-190. [10.1007/s10725-021-00735-3]

The adjuvant activity of two urea derivatives on cytokinins: an example of serendipitous dual effect

Brunoni F.
Membro del Collaboration Group
;
Rolli E.
Membro del Collaboration Group
;
Polverini E.
Membro del Collaboration Group
;
Ricci A.
Membro del Collaboration Group
2021

Abstract

The aim of this study was to investigate the action spectrum of two urea derivatives, the 1,3-di(benzo[d]oxazol-5-yl)urea (5-BDPU) and the 1,3-di(benzo[d]oxazol-6-yl)urea (6-BDPU). In order to evaluate a possible adjuvant activity on cytokinins the compounds alone or in the simultaneous presence of different cytokinins were assayed either on in vitro typical cytokinin-related bioassays, or on in planta interaction with cytokinin signal transduction pathway. The compounds ability to activate the cytokinin receptor CRE1/AHK4 was studied either by a heterologous bacterial assay or by a competitive binding assay and docking simulations were performed with the crystal structure of the same receptor. Then, owing to their chemical structure which resembles that of urea-type cytokinins, the ability of 5- and 6-BDPU to inhibit the activity of cytokinin oxidase/dehydrogenase of Zea mays (ZmCKX1) was investigated and docking simulations were performed as well. Accordingly to the experimental results, we speculate that BDPUs could show a dual activity: the blocking of the conformational re-adaption of CRE1/AHK4 receptor maintaining the cytokinin inside its binding pocket, thus possibly enhancing its kinase action; the inhibition of cytokinin oxidase/dehydrogenase activity thus possibly preventing its cleavage of natural cytokinins with isoprenoid side chain. Graphic abstract: [Figure not available: see fulltext.]
The adjuvant activity of two urea derivatives on cytokinins: an example of serendipitous dual effect / Brunoni, F.; Rolli, E.; Polverini, E.; Spichal, L.; Ricci, A.. - In: PLANT GROWTH REGULATION. - ISSN 0167-6903. - 95:(2021), pp. 169-190. [10.1007/s10725-021-00735-3]
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Utilizza questo identificativo per citare o creare un link a questo documento: https://hdl.handle.net/11381/2897458
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