Dynamic control of plant water use using designed ABA receptor agonists
Dynamic control of plant water use using designed ABA receptor agonists
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DOI：
10.1126/science.aaw8848
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发表时间：
2019-10-25
期刊：
影响因子：
56.9
通讯作者：
Cutler, Sean R.
中科院分区：
文献类型：
--
作者：
Vaidya, Aditya S.;Helander, Jonathan D. M.;Cutler, Sean R.
干旱导致全球农作物损失，随着全球变暖，其影响预计会增加。这推动了小分子工具的开发，以减轻干旱对农业的影响。我们在这里表明，目前的铅受到小麦（一种广泛种植的主要作物）和番茄的生物活性差的限制。为了解决这一局限性，我们结合虚拟筛选、x射线晶体学和结构引导设计开发了opabactin (OP)，这是一种脱落酸（ABA）模拟物，与ABA相比，受体亲和力增加了约7倍，体内活性提高了10倍。在拟南芥中的研究揭示了III型受体PYRABACTIN RESISTANCE-LIKE 2在op抗蒸发功效中的作用。因此，虚拟筛选和结构导向优化产生了新发现的激动剂，可用于控制作物的非生物胁迫耐受性和水分利用。
Drought causes crop losses worldwide, and its impact is expected to increase as the world warms. This has motivated the development of small-molecule tools for mitigating the effects of drought on agriculture. We show here that current leads are limited by poor bioactivity in wheat, a widely grown staple crop, and in tomato. To address this limitation, we combined virtual screening, x-ray crystallography, and structure-guided design to develop opabactin (OP), an abscisic acid (ABA) mimic with up to an approximately sevenfold increase in receptor affinity relative to ABA and up to 10-fold greater activity in vivo. Studies in Arabidopsis thaliana reveal a role of the type III receptor PYRABACTIN RESISTANCE-LIKE 2 for the antitranspirant efficacy of OP. Thus, virtual screening and structure-guided optimization yielded newly discovered agonists for manipulating crop abiotic stress tolerance and water use.