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具有不同烷基链长度的脱落酸衍生物激活不同的脱落酸受体亚家族。

Abscisic Acid Derivatives with Different Alkyl Chain Lengths Activate Distinct Abscisic Acid Receptor Subfamilies.

机构信息

Chemical Biology Research Group , RIKEN Center for Sustainable Resource Science , 2-1 Hirosawa , Wako , Saitama 351-0198 , Japan.

Health & Crop Sciences Research Laboratory , Sumitomo Chemical Co., Ltd. , 4-2-1 Takarazuka , Hyogo 665-8555 , Japan.

出版信息

ACS Chem Biol. 2019 Sep 20;14(9):1964-1971. doi: 10.1021/acschembio.9b00453. Epub 2019 Sep 9.

Abstract

The plant hormone abscisic acid (ABA) regulates the development of various plant organs including seeds, roots, and fruits, and significantly contributes to abiotic stress responses, especially to drought. Since recent climate changes are adversely affecting crop cultivation, enhancement of plant stress tolerance by regulation of ABA signaling would be an important strategy. In the plant genome, ABA receptors are encoded by multiple genes constituting three subfamilies; however, functional differences among them remain unclear. To enhance desired effects of ABA, the biological functions of the receptor family warrant clarification. This study aimed to determine the functional differences among ABA receptors in plants. We screened small-molecule ligands binding to specific receptors, using a chemical array. evaluation of hit compounds using 11 ABA receptors revealed that (+)-3'-alkyl ABAs served as agonists for different receptors depending on the length of their 3'-alkyl chains. Combinatorial and physiological effects of these compounds on the stomata, seeds, and seedlings indicated that, along with subfamily III, receptors of subfamily II are important to induce strong drought responses. Among (+)-3'-alkyl ABAs assessed herein, (+)-3'-butyl ABA induced a transcriptional response and stomatal closure but only slightly inhibited seed germination and growth, suggesting that it enhances drought tolerance. In silico docking simulation and site-directed mutagenesis revealed the amino acid residues contributing to the selective agonist activity of the (+)-3'-alkyl ABAs. These results provide novel insights into the structure and biological effects of 3'-derivatives of ABA and a basis for agrochemical development.

摘要

植物激素脱落酸(ABA)调节各种植物器官的发育,包括种子、根和果实,并显著促进非生物胁迫反应,特别是干旱。由于最近的气候变化对作物种植产生不利影响,通过调节 ABA 信号来增强植物的胁迫耐受性将是一个重要策略。在植物基因组中,ABA 受体由构成三个亚家族的多个基因编码;然而,它们之间的功能差异尚不清楚。为了增强 ABA 的预期效果,有必要阐明受体家族的生物学功能。本研究旨在确定植物中 ABA 受体的功能差异。我们使用化学阵列筛选与特定受体结合的小分子配体。对 11 种 ABA 受体的命中化合物进行评估表明,(+)-3'-烷基 ABA 作为不同受体的激动剂,具体取决于其 3'-烷基链的长度。这些化合物对气孔、种子和幼苗的组合和生理效应表明,除了亚家族 III 外,亚家族 II 的受体对于诱导强烈的干旱反应也很重要。在本文评估的(+)-3'-烷基 ABA 中,(+)-3'-丁基 ABA 诱导了转录反应和气孔关闭,但仅轻微抑制种子萌发和生长,表明其增强了耐旱性。计算机对接模拟和定点突变揭示了决定(+)-3'-烷基 ABA 选择性激动剂活性的氨基酸残基。这些结果为 ABA 的 3'-衍生物的结构和生物学效应提供了新的见解,并为农用化学品的开发提供了基础。

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