Cytokinin oxidase/dehydrogenase inhibitors: outlook for selectivity and high efficiency
العنوان: | Cytokinin oxidase/dehydrogenase inhibitors: outlook for selectivity and high efficiency |
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المؤلفون: | Jaroslav Nisler, Zuzana Pěkná, Radka Končitíková, Pavel Klimeš, Alena Kadlecová, Nino Murvanidze, Stefaan P O Werbrouck, Lenka Plačková, David Kopečný, David Zalabák, Lukáš Spíchal, Miroslav Strnad |
المصدر: | Journal of Experimental Botany. 73:4806-4817 |
بيانات النشر: | Oxford University Press (OUP), 2022. |
سنة النشر: | 2022 |
مصطلحات موضوعية: | Cytokinins, Physiology, Arabidopsis, Plant Science, Plants, Oxidoreductases, Zea mays |
الوصف: | Inhibitors of cytokinin oxidase/dehydrogenase (CKX) reduce the degradation of cytokinins in plants, and this effect can be exploited in agriculture and in plant tissue culture. In this study, we examine the structure–activity relationship of two series of CKX inhibitors based on diphenylurea. The compounds of Series I were derived from the recently published CKX inhibitors 3TFM-2HM and 3TFM-2HE, and we identified key substituents with increased selectivity for maize ZmCKX1 and ZmCKX4a over AtCKX2 from Arabidopsis. Series II contained compounds that further exceled in CKX inhibitory activity as well as in the ease of their synthesis. The best inhibitors exhibited half-maximal inhibitory concentration (IC50) values in low nanomolar ranges with ZmCKX1 and especially with ZmCKX4a, which is generally more resistant to inhibition. The activity of the key compounds was verified in tobacco and lobelia leaf-disk assays, where N6-isopentenyladenine was protected from degradation and promoted shoot regeneration. All the prepared compounds were further tested for toxicity against Caenorhabditis elegans, and the assays revealed clear differences in toxicity between compounds with and without a hydroxyalkyl group. In a broader perspective, this work increases our understanding of CKX inhibition and provides a more extensive portfolio of compounds suitable for agricultural and biotechnological research. |
تدمد: | 1460-2431 0022-0957 |
URL الوصول: | https://explore.openaire.eu/search/publication?articleId=doi_dedup___::23fbd27409a675ecf9b53555a3956b9b https://doi.org/10.1093/jxb/erac201 |
حقوق: | CLOSED |
رقم الأكسشن: | edsair.doi.dedup.....23fbd27409a675ecf9b53555a3956b9b |
قاعدة البيانات: | OpenAIRE |
تدمد: | 14602431 00220957 |
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