{"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}
引用次数: 0
Abstract
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.