Cytokinin oxidase/dehydrogenase inhibitors: progress towards agricultural practice
2024
Nisler, Jaroslav | Klimeš, Pavel | Končitíková, Radka | Kadlecová, Alena | Voller, Jiří | Chalaki, Mahfam | Karampelias, Michael | Murvanidze, Nino | Werbrouck, Stefaan, P O | Kopečný, David | Havlíček, Libor | de Diego, Nuria | Briozzo, Pierre | Moréra, Solange | Zalabák, David | Spíchal, Lukáš | Institute of Experimental Botany of the Czech Academy of Sciences (IEB / CAS) ; Czech Academy of Sciences [Prague] (CAS) | Palacky University Olomouc | Faculty of Science [Univ Palacký] ; Palacky University Olomouc | Přírodovědecká fakulta, Univerzita Karlova [Praha, Česká republika] = Faculty of Sciences, Charles University [Prague, Czech Republic] (PřF UK) ; Univerzita Karlova [Praha, Česká republika] = Charles University [Prague, Czech Republic] (UK) | Faculty of Bioscience Engineering [Ghent] ; Universiteit Gent = Ghent University = Université de Gand (UGENT) | Institut Jean-Pierre Bourgin - Sciences du végétal (IJPB) ; AgroParisTech-Université Paris-Saclay-Institut National de Recherche pour l’Agriculture, l’Alimentation et l’Environnement (INRAE) | Institut de Biologie Intégrative de la Cellule (I2BC) ; Commissariat à l'énergie atomique et aux énergies alternatives (CEA)-Université Paris-Saclay-Centre National de la Recherche Scientifique (CNRS) | grant no. 21-07661S from the Czech Science Foundation | Czech Science Foundation project number 21-20936J and the HORIZON-WIDERA-2022-TALENTS-02 project number 101090293 | ANR-11-IDEX-0003,IPS,Idex Paris-Saclay(2011)
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Mostrar más [+] Menos [-]Inglés. Abstract Cytokinin oxidase/dehydrogenase (CKX) inhibitors reduce the degradation of cytokinins in plants and thereby may improve the efficiency of agriculture and plant tissue culture-based practices. Here, we report a synthesis and structure–activity relationship study of novel urea derivatives concerning their CKX inhibitory activity. The most active compounds showed sub-nanomolar IC50 values with maize ZmCKX1, the lowest value yet documented. Other CKX isoforms of maize and Arabidopsis were also inhibited very effectively. The binding mode of four compounds was characterized based on high-resolution crystal complex structures. Using the soil nematode Caenorhabditis elegans, and human skin fibroblasts, key CKX inhibitors with low toxicity were identified. These compounds enhanced the shoot regeneration of Lobelia, Drosera, and Plectranthus, as well as the growth of Arabidopsis and Brassica napus. At the same time, a key compound (identified as 82) activated a cytokinin primary response gene, ARR5:GUS, and a cytokinin sensor, TCSv2:GUS, without activating the Arabidopsis cytokinin receptors AHK3 and AHK4. This strongly implies that the effect of compound 82 is due to the up-regulation of cytokinin signalling. Overall, this study identifies highly effective and easily prepared CKX inhibitors with a low risk of environmental toxicity for further investigation of their potential in agriculture and biotechnology.
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