Substituted Phthalimide AC94377 Is a Selective Agonist of the Gibberellin Receptor GID1
Substituted Phthalimide AC94377 Is a Selective Agonist of the Gibberellin Receptor GID1
复制标题
DOI：
10.1104/pp.16.00937
复制
发表时间：
2017-01-01
期刊：
影响因子：
7.4
通讯作者：
Asami, Tadao
中科院分区：
文献类型：
--
作者：
Jiang, Kai;Otani, Masato;Asami, Tadao
赤霉素（GA）是一种调节植物生长发育的主要植物激素，作为植物生长调节剂广泛应用于农业生产中。由于GA对作物的农学应用的限制，包括GA的高生产成本及其导致作物倒伏，对功能有限的GA模拟物的需求日益增加。AC 94377是一种取代的邻苯二甲酰亚胺，是一种模拟各种植物中GA生长调节活性的化学物质，尽管其结构不同。虽然AC 94377在许多杂草和作物中被广泛研究，但其作为GA模拟物的作用模式在很大程度上是未知的。在这项研究中，我们证实了AC 94377在拟南芥（Arabidopsis thaliana）中表现出GA样活性，并证明AC 94377与拟南芥赤霉素不敏感性DWARF 1（GID 1）受体（AtGID 1）结合，形成AtGID 1-AC 94377- DELLA复合物，并诱导DELLA蛋白降解。我们的研究结果还表明，AC 94377是选择性的一个特定的亚型之间的三个AtGID 1和AC 94377的选择性是由于一个单一的残基在入口处的疏水口袋的GID 1。我们的结论是，AC 94377是一种具有选择性的GID 1激动剂的特定亚型的GID 1，这可以进一步开发，并作为一个功能有限的植物生长调节剂在基础研究和农业。
Gibberellin (GA) is a major plant hormone that regulates plant growth and development and is widely used as a plant growth regulator in agricultural production. There is an increasing demand for function-limited GA mimics due to the limitations on the agronomical application of GA to crops, including GA's high cost of producing and its leading to the crops' lodging. AC94377, a substituted phthalimide, is a chemical that mimics the growth-regulating activity of GAs in various plants, despite its structural difference. Although AC94377 is widely studied in many weeds and crops, its mode of action as a GA mimic is largely unknown. In this study, we confirmed that AC94377 displays GA-like activities in Arabidopsis (Arabidopsis thaliana) and demonstrated that AC94377 binds to the Arabidopsis GIBBERELLIN INSENSITIVE DWARF1 (GID1) receptor (AtGID1), forms the AtGID1-AC94377- DELLA complex, and induces the degradation of DELLA protein. Our results also indicated that AC94377 is selective for a specific subtype among three AtGID1s and that the selectivity of AC94377 is attributable to a single residue at the entrance to the hydrophobic pocket of GID1. We conclude that AC94377 is a GID1 agonist with selectivity for a specific subtype of GID1, which could be further developed and used as a function-limited regulator of plant growth in both basic study and agriculture.