Takeuchi Jun, Ohnishi Toshiyuki, Okamoto Masanori, Todoroki Yasushi
Graduate School of Agriculture, Shizuoka University, 836 Ohya, Suruga-ku, Shizuoka 422-8529, Japan.
Graduate School of Agriculture, Shizuoka University, 836 Ohya, Suruga-ku, Shizuoka 422-8529, Japan; Research Institute of Green Science and Technology, Shizuoka University, 836 Ohya, Suruga-ku, Shizuoka 422-8529, Japan.
Bioorg Med Chem Lett. 2015 Sep 1;25(17):3507-10. doi: 10.1016/j.bmcl.2015.06.088. Epub 2015 Jul 3.
Abscisic acid (ABA), a plant hormone, is involved in many plant development processes and environmental stress responses that are regulated by a Pyrabactin Resistant 1 (PYR)/Pyrabactin Resistant-Like (PYL)/Regulatory Component of ABA Receptor (RCAR) receptor protein-mediated signal transduction pathway. In Arabidopsis thaliana, PYL proteins constitute a 14-member family comprising two distinct subclasses: dimeric receptors (PYR1 and PYL1-PYL3) and monomeric receptors (PYL4-PYL13). The individual contributions of PYL subclasses/subtypes with specific physiological actions are still poorly understood; consequently, the development of PYL subclass/subtype-selective agonists should be useful to reveal the different functions of these receptors. In this study, we focused on the ABA analogs 6-nor-ABA and 7'-nor-ABA, which were expected to function as monomeric receptor-selective agonists on the basis of crystal structures of PYL-ABA complexes and sequence alignments of PYL subtypes. In a protein phosphatase 2C (PP2C) assay, the agonist activities of both analogs were lower than those of ABA toward all tested PYL proteins, regardless of subclass/subtype. Nevertheless, we found that 6-nor-ABA acts as a selective agonist at the physiological level: it induced stomatal closure but did not inhibit seed germination and root growth. On the basis of observed inhibitory activity against PP2C among different PYL subtypes, this biological effect of 6-nor-ABA may be attributed to the activity of that agonist on PYL5 and/or PYL6.
脱落酸(ABA)是一种植物激素,参与许多植物发育过程和环境胁迫反应,这些过程和反应由吡唑啉酮抗性1(PYR)/类吡唑啉酮抗性(PYL)/ABA受体调节成分(RCAR)受体蛋白介导的信号转导途径调控。在拟南芥中,PYL蛋白构成一个由14个成员组成的家族,包括两个不同的亚类:二聚体受体(PYR1和PYL1 - PYL3)和单体受体(PYL4 - PYL13)。PYL亚类/亚型的具体生理作用的个体贡献仍知之甚少;因此,开发PYL亚类/亚型选择性激动剂有助于揭示这些受体的不同功能。在本研究中,我们聚焦于ABA类似物6 - 去甲ABA和7'-去甲ABA,基于PYL - ABA复合物的晶体结构和PYL亚型的序列比对,预计它们可作为单体受体选择性激动剂。在蛋白磷酸酶2C(PP2C)测定中,无论亚类/亚型如何,这两种类似物对所有测试的PYL蛋白的激动剂活性均低于ABA。然而,我们发现6 - 去甲ABA在生理水平上作为一种选择性激动剂:它诱导气孔关闭,但不抑制种子萌发和根生长。基于在不同PYL亚型中观察到的对PP2C的抑制活性,6 - 去甲ABA的这种生物学效应可能归因于该激动剂对PYL5和/或PYL6的活性。