Chen Meng, Yang Zhisen, Peng Yakun, Sun Lianghanxiao, Liu Xin, Sun Linfeng, Tan Shutang
Ministry of Education Key Laboratory for Membraneless Organelles and Cellular Dynamics, Center for Advanced Interdisciplinary Science and Biomedicine of Institute of Health and Medicine, Hefei National Laboratory for Physical Sciences at the Microscale, Division of Life Sciences and Medicine, University of Science and Technology of China, Hefei, China.
Front Plant Sci. 2025 Mar 12;16:1563571. doi: 10.3389/fpls.2025.1563571. eCollection 2025.
The phytohormone auxin plays a central role in plant growth and development. D6PK, a member of the AGC kinase family, phosphorylates PIN-FORMED (PIN) auxin transporters, thereby regulating PIN activity and polar auxin transport. In this study, we demonstrated that gravacin, a synthetic compound, functions as an inhibitor that targets D6PK in plants. Physiological and cell biology experiments revealed that the phenotypes of gravacin-treated plants were similar to those of triple mutants. Furthermore, kinase assays confirmed that gravacin directly inhibited the kinase activity of D6PK. Thus, by combining phenotypic analysis with cell biological and biochemical experiments, this research revealed that gravacin is an inhibitor of D6PK and elucidated the underlying mechanism. Our work provides a chemical tool that can be used to further dissect the role of D6PK and related physiological processes.
植物激素生长素在植物生长发育中起核心作用。D6PK是AGC激酶家族的一员，可磷酸化生长素输出载体PIN，从而调节PIN活性和生长素极性运输。在本研究中，我们证明了合成化合物gravacin在植物中作为靶向D6PK的抑制剂发挥作用。生理和细胞生物学实验表明，gravacin处理的植物表型与三重突变体相似。此外，激酶分析证实gravacin直接抑制D6PK的激酶活性。因此，通过将表型分析与细胞生物学和生化实验相结合，本研究揭示了gravacin是D6PK的抑制剂，并阐明了其潜在机制。我们的工作提供了一种化学工具，可用于进一步剖析D6PK的作用及相关生理过程。
