Screening of protonstatin-1 (PS-1) analogs for improved inhibitors of plant plasma membrane H(+)-ATPase activity.
Screening of protonstatin-1 (PS-1) analogs for improved inhibitors of plant plasma membrane H(+)-ATPase activity.
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筛选质子抑素-1 (PS-1) 类似物以改善植物质膜 H-ATP 酶活性抑制剂
DOI：
10.3389/fpls.2022.973471
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发表时间：
2022
影响因子：
5.6
通讯作者：
中科院分区：
文献类型：
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我们先前发现Protonstatin-1(PS-1)是质膜H+-ATPase(PM H+-ATPase)活性的选择性抑制物，并将其用作验证生长素极性运输的化学渗透模型的工具。在这里，为了获得比PS-1对PM H+-ATPase具有更高亲和力的化合物，我们合成了34个PS-1类似物，并检测了它们对PM H+-ATPase活性的抑制能力。34个类似物对该酶有不同程度的抑制作用。小分子PS-2的作用最强，大约是PS-1的五倍。与PS-1相比，PS-2对拟南芥幼苗生长素的吸收以及顶瓣和基瓣的生长素运输具有更强的抑制作用。由于PS-2是一种比PS-1更有效的质膜H+-ATPase抑制剂，我们认为该化合物可以作为研究这一关键植物酶功能的工具。
We previously identified protonstatin-1 (PS-1) as a selective inhibitor of plasma membrane H+-ATPase (PM H+-ATPase) activity and used it as a tool to validate the chemiosmotic model for polar auxin transport. Here, to obtain compounds with higher affinity than PS-1 for PM H+-ATPase, we synthesized 34 PS-1 analogs and examined their ability to inhibit PM H+-ATPase activity. The 34 analogs showed varying inhibitory effects on the activity of this enzyme. The strongest effect was observed for the small molecule PS-2, which was approximately five times stronger than PS-1. Compared to PS-1, PS-2 was also a stronger inhibitor of auxin uptake as well as acropetal and basipetal polar auxin transport in Arabidopsis thaliana seedlings. Because PS-2 is a more potent inhibitor of PM H+-ATPase than PS-1, we believe that this compound could be used as a tool to study the functions of this key plant enzyme.