{"title":"格拉星对拟南芥生长素转运激活蛋白激酶D6PK的抑制作用。","authors":"Meng Chen, Zhisen Yang, Yakun Peng, Lianghanxiao Sun, Xin Liu, Linfeng Sun, Shutang Tan","doi":"10.3389/fpls.2025.1563571","DOIUrl":null,"url":null,"abstract":"<p><p>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 <i>d6pk d6pkl1 d6pkl2 (d0 d1 d2)</i> triple mutants. Furthermore, <i>in vitro</i> 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.</p>","PeriodicalId":12632,"journal":{"name":"Frontiers in Plant Science","volume":"16 ","pages":"1563571"},"PeriodicalIF":4.1000,"publicationDate":"2025-03-12","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"https://www.ncbi.nlm.nih.gov/pmc/articles/PMC11938129/pdf/","citationCount":"0","resultStr":"{\"title\":\"Gravacin as an inhibitor of the auxin transport-activating protein kinase D6PK in <i>Arabidopsis</i>.\",\"authors\":\"Meng Chen, Zhisen Yang, Yakun Peng, Lianghanxiao Sun, Xin Liu, Linfeng Sun, Shutang Tan\",\"doi\":\"10.3389/fpls.2025.1563571\",\"DOIUrl\":null,\"url\":null,\"abstract\":\"<p><p>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 <i>d6pk d6pkl1 d6pkl2 (d0 d1 d2)</i> triple mutants. Furthermore, <i>in vitro</i> 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.</p>\",\"PeriodicalId\":12632,\"journal\":{\"name\":\"Frontiers in Plant Science\",\"volume\":\"16 \",\"pages\":\"1563571\"},\"PeriodicalIF\":4.1000,\"publicationDate\":\"2025-03-12\",\"publicationTypes\":\"Journal Article\",\"fieldsOfStudy\":null,\"isOpenAccess\":false,\"openAccessPdf\":\"https://www.ncbi.nlm.nih.gov/pmc/articles/PMC11938129/pdf/\",\"citationCount\":\"0\",\"resultStr\":null,\"platform\":\"Semanticscholar\",\"paperid\":null,\"PeriodicalName\":\"Frontiers in Plant Science\",\"FirstCategoryId\":\"99\",\"ListUrlMain\":\"https://doi.org/10.3389/fpls.2025.1563571\",\"RegionNum\":2,\"RegionCategory\":\"生物学\",\"ArticlePicture\":[],\"TitleCN\":null,\"AbstractTextCN\":null,\"PMCID\":null,\"EPubDate\":\"2025/1/1 0:00:00\",\"PubModel\":\"eCollection\",\"JCR\":\"Q1\",\"JCRName\":\"PLANT SCIENCES\",\"Score\":null,\"Total\":0}","platform":"Semanticscholar","paperid":null,"PeriodicalName":"Frontiers in Plant Science","FirstCategoryId":"99","ListUrlMain":"https://doi.org/10.3389/fpls.2025.1563571","RegionNum":2,"RegionCategory":"生物学","ArticlePicture":[],"TitleCN":null,"AbstractTextCN":null,"PMCID":null,"EPubDate":"2025/1/1 0:00:00","PubModel":"eCollection","JCR":"Q1","JCRName":"PLANT SCIENCES","Score":null,"Total":0}
引用次数: 0
摘要
植物激素生长素在植物生长发育中起着重要作用。D6PK是AGC激酶家族的一员，磷酸化PIN- formed （PIN）生长素转运蛋白，从而调节PIN活性和极性生长素运输。在这项研究中，我们证明了格拉星是一种合成化合物，在植物中作为一种靶向D6PK的抑制剂。生理和细胞生物学实验表明，经gravacin处理的植株表型与d6pk d6pkl1 d6pkl2 （d0 d1 d2）三突变体相似。此外，体外激酶实验证实，格拉星直接抑制D6PK的激酶活性。因此，本研究通过表型分析和细胞生物学生化实验相结合，揭示了格拉星是D6PK的抑制剂，并阐明了其作用机制。我们的工作提供了一个化学工具，可以用来进一步剖析D6PK的作用和相关的生理过程。
Gravacin as an inhibitor of the auxin transport-activating protein kinase D6PK in Arabidopsis.
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 d6pk d6pkl1 d6pkl2 (d0 d1 d2) triple mutants. Furthermore, in vitro 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.
期刊介绍：
In an ever changing world, plant science is of the utmost importance for securing the future well-being of humankind. Plants provide oxygen, food, feed, fibers, and building materials. In addition, they are a diverse source of industrial and pharmaceutical chemicals. Plants are centrally important to the health of ecosystems, and their understanding is critical for learning how to manage and maintain a sustainable biosphere. Plant science is extremely interdisciplinary, reaching from agricultural science to paleobotany, and molecular physiology to ecology. It uses the latest developments in computer science, optics, molecular biology and genomics to address challenges in model systems, agricultural crops, and ecosystems. Plant science research inquires into the form, function, development, diversity, reproduction, evolution and uses of both higher and lower plants and their interactions with other organisms throughout the biosphere. Frontiers in Plant Science welcomes outstanding contributions in any field of plant science from basic to applied research, from organismal to molecular studies, from single plant analysis to studies of populations and whole ecosystems, and from molecular to biophysical to computational approaches.
Frontiers in Plant Science publishes articles on the most outstanding discoveries across a wide research spectrum of Plant Science. The mission of Frontiers in Plant Science is to bring all relevant Plant Science areas together on a single platform.
求助内容：
应助结果提醒方式：
京公网安备 11010802042870号
