Development of phloem-mobile xenobiotics with enhanced transport properties

每年，农用化学品行业都会筛选数千种化学品，以确定其作为除草剂和杀虫剂的潜在用途。这些化合物很少进入市场，因为它们不能有效地进入或移动到植物组织中。给定分子进入植物内部传导系统韧皮部的能力是开发成功的内吸性除草剂的主要障碍。草甘膦（Roundup）在世界范围内的成功主要是由于这种化学物质在韧皮部中非常有效地移动，因此能够对远处生长的组织产生毒性作用。与许多其他除草剂不同，Glycoprotein似乎使用植物膜载体蛋白进行有效运输。该项目的目的是开发新一代化学品，旨在有效地在韧皮部中移动。化学品现场应用所伴随的径流是一个相当大的环境问题，因为这些潜在有毒化学品中的一些可能污染蒸汽和水道。很明显，开发新的化学品，通过更有效的运输到达目标地点，将是这一领域的一个主要优势，减少需要施用于作物的数量，从而最大限度地减少径流。因此，本项目的直接目标是通过合理设计具有增强韧皮部移动性的新化学品来改善农用化学品在植物中的移动。该项目采用了一种新的方法，即使用专门设计用于在植物韧皮部移动的荧光探针。使用基于荧光的化学品意味着可以使用适当的荧光检测方法（例如荧光显微镜）详细研究吸收和转运过程。一个主要的目标是使用现有的蛋白质将这些荧光化合物中的一些“背驮”到韧皮部中，这些蛋白质的功能是在韧皮部中运输天然化合物。

Every year, several thousand chemicals are screened by the agrochemical industry for potential uses as herbicides and pesticides. Very few of these compounds make it to the market place because they do not enter or move in plant tissues effectively. The ability of a given molecule to enter the phloem, the plant's internal conducting system, is a major hurdle to the development of successful systemic herbicides. The worldwide success of Glyphosate (Roundup) is due predominantly to the fact that this chemical moves extremely effectively in the phloem and is therefore able to exert its toxic effects on distant growing tissues. Unlike many other herbicides, Glyphosate appears to use plant membrane carrier proteins for its effective transport. The aim of this project is to develop new-generation chemicals that are designed to move effectively in the phloem.The run-off that accompanies field applications of chemicals is a matter of considerable environmental concern as several of these potentially toxic chemicals may pollute steams and waterways. It is clear that the development of new chemicals that reach their target sites by more efficient transport would be a major advantage in this field, reducing the amounts that need to be applied to crops and thereby minimizing run-off. This project is therefore aimed directly at improving the movement of agrochemicals in plants by the rational design of new chemicals that show enhanced phloem-mobility properties.The project takes a novel approach by using fluorescent probes that are designed specifically to move in the phloem of plants. Using fluorescence-based chemicals means that the process of uptake and transport can be studied in fine detail using appropriate fluorescence detection methods (e.g. fluorescence microscopy). A major goal is to 'piggy back' some of these fluorescent compounds into the phloem using existing proteins that function to transport natural compounds in the phloem.