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245 1 0 _aCytokinin oxidase/dehydrogenase inhibitors: progress towards agricultural practice
490 0 _aJournal of Experimental Botany. 75(16), 4873-4890, 2024, DOI: 10.1093/jxb/erae239
520 3 _aCytokinin 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. © The Author(s) 2024
650 1 4 _aAGRICULTURE
650 1 4 _aARABIDOPSIS
650 1 4 _aBIOSTIMULANT
650 1 4 _aBIOTECHNOLOGY
650 1 4 _aCKX INHIBITOR
650 1 4 _aCYTOKININ
650 1 4 _aCYTOKININ OXIDASE/DEHYDROGENASE
650 1 4 _aDIPHENYLUREA
650 1 4 _aNUTRIENT USE EFFICIENCY
650 1 4 _aOILSEED RAPE
700 1 2 _aNisler J.
700 1 2 _aKlimeš P.
700 1 2 _aKon?itíková R.
700 1 2 _aKadlecová A.
700 1 2 _aVoller J.
700 1 2 _aChalaki M.
700 1 2 _aKarampelias M.
700 1 2 _aMurvanidze N.
700 1 2 _aWerbrouck S.P.O.
700 1 2 _aKope?ný D.
700 1 2 _aHavlí?ek L.
700 1 2 _aDe Diego N.
700 1 2 _aBriozzo P.
700 1 2 _aMoréra S.
700 1 2 _aZalabák D.
700 1 2 _aSpíchal L.
856 4 0 _uhttps://drive.google.com/file/d/1Swf68ZqiP0Xtrhg9UvWv6DS-h2zefvwy/view?usp=drivesdk
_zPara ver el documento ingresa a Google con tu cuenta @cicy.edu.mx
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