Receptor-like kinases (RLKs) constitute the largest receptor family involved in the regulation of plant immunity and growth, but small-molecule inhibitors that target RLKs to improve agronomic traits remain unexplored. The RLK member FERONIA (FER) negatively regulates plant resistance to certain soil-borne diseases that are difficult to control and cause huge losses in crop yields and economy. Here, we identified 33 highly effective FER kinase inhibitors from 1494 small molecules by monitoring FER autophosphorylation in vitro. Four representative inhibitors (reversine, cenisertib, staurosporine and lavendustin A) inhibited the kinase activity of FER and its homologues in several crops by targeting the conserved ATP pocket in the kinase structure. FER contributes to the physiological impact of representative inhibitors in plants. The treatment of roots with reversine, staurosporine and lavendustin A enhanced innate immunity in plant roots and thus alleviated soil-borne diseases in tobacco, tomato and rice without growth penalties. Consistently, RNA sequencing assays showed that lavendustin A and reversine exert profound impacts on immunity-related gene expression. Our results will set a new milestone in the development of the plant RLK kinase regulation theory and provide a novel strategy for the prevention and control of plant soil-borne diseases without growth penalties.

中文翻译：

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针对受体激酶 FERONIA 的抑制剂筛选揭示了增强植物根部免疫力的小分子


类受体激酶 (RLK) 构成了参与植物免疫和生长调节的最大受体家族，但针对 RLK 来改善农艺性状的小分子抑制剂仍未得到探索。 RLK成员FERONIA（FER）对植物对某些难以控制的土传病害的抗性进行负调控，对作物产量和经济造成巨大损失。在这里，我们通过体外监测 FER 自磷酸化，从 1494 个小分子中鉴定出了 33 种高效的 FER 激酶抑制剂。四种代表性抑制剂（reversine、cenisertib、staurosporine 和 lavendustin A）通过靶向激酶结构中的保守 ATP 袋来抑制几种作物中 FER 及其同系物的激酶活性。 FER 有助于植物中代表性抑制剂的生理影响。用逆转素、十字孢菌素和薰衣草素 A 处理根部可增强植物根部的先天免疫力，从而减轻烟草、番茄和水稻的土传病害，且不会影响生长。 RNA 测序分析一致表明，薰衣草素 A 和逆碱对免疫相关基因表达具有深远影响。我们的研究结果将为植物RLK激酶调控理论的发展树立一个新的里程碑，并为预防和控制植物土传病害提供一种新的策略，而不会影响生长。