China丨Hundreds of new pesticides are expected to emerge

Pesticides arestrategic materials which can ensure the food security. Without pesticides,crops would be reduced by more than 30 % every year. The safe and eco-friendlypesticides are essential for food security, people health and sustainabledevelopment of agriculture.

Bring billions of dollars to the market

on Sept 21,Professor Yang Qing's team from IPP·CAAS/ AGIS·CAAS and his collaborators published the research onlinein the internationally renowned academic journal “Nature”. It almost took his 15 years tocomplete this research. This paper studied Cryo-EM structure of Chitinsynthetase from Phytophthorasojae. It revealedfor the first time the complete process of Chitin biosynthesis, including threesteps: binding of enzyme to substrate, extension of newly generated Chitin chain, and release of product. Themechanism of inhibiting Chitin biosynthesis by Nikkomycins was elucidated.

In recentyears, this paper is one of the most important basic research advances in theglobal pesticide field.

This workprovides key information for the development of green pesticides targetingChitin synthesis and makes the precise development of new green pesticidesusing Chitinsynthetase as moleculartarget to be a scientific and feasible scheme, which has important theoreticaland application value.

This researchis also regarded as a milestone in the field of pesticide research, achieving abreakthrough in the basic research of pesticides and illuminating the prospectof precise design of new green pesticides. Based on this research, dozens oreven hundreds of new pesticides may be created in the future, bringing billionsof dollars to the market.

New green pesticides are needed by industry

The use ofpesticides reduces the direct economic losses about 100 billion yuan every yearin China, but pesticide toxicity and resistance to pests and diseases make it aserious challenge in many ways. Accelerating the R&D of pesticides withsafe andnew mode of action is an effective way to solve the problem.

The core ofthe scientific problem lies in the molecular targets of pesticides, that is, thebiological macromolecules that bind the pesticide molecules in the body ofpests and diseases to make the pesticide molecules exert their effects.

At present,70% of the widely used insecticides in the world target only 5 moleculartargets, and 60% of the widely used fungicides target only 3 targets.

Long-term useof pesticides, which target a single target, will easily lead to highresistance of pests and diseases, and eventually lead to the failure ofpesticides to control the population of pests and diseases, resulting infrequent outbreaks of pests and diseases. This is also a major problem faced byglobal agriculture for pest control.

Chitin is anatural biopolymer composed of N-acetyl-D-(+)-glucosamine, and its biosynthesisis essential to the survival and reproduction of a large number of organisms,including many pests, Pathogenic fungi and Oomycetes that seriously harmagricultural production.

Chitin is notfound in plants and mammals, so Chitin synthetase is one of the importanttargets for the development of efficient and eco-friendly pesticides.

Since the1970s, human have successively developed the compounds which can inhibit thesynthesis of chitin. These compounds also have shown great application and marketprospect as fungicides and insecticides.

However, inthe past 50 years, despite a lot of human resources and enthusiasm, countriesaround the world have been trying to develop more types and more efficientgreen pesticides, but progress has been slow. One of the important reasons isthe lack of accurate three-dimensional structural information of Chitinsynthetase. The structure-function relationship of Chitin synthetase is notclear, which seriously hinders the design of new pesticides for this enzyme.

Break through the bottleneck of Chitin pesticide’s development

Yang has beendevoted to the research of Chitin biology for a long time, and has accumulatedabundant knowledge in the synthesis, hydrolysis and modification of Chitin.

The resultsprovide the key information of molecular target structure for the developmentof safe green pesticides for human and livestock and provide a new solution forthe control of resistance of pests and diseases to existing pesticides.

Qian from CAEpointed out that the study has broken through a nearly 50-year developmentbottleneck in the field of chitin pesticides. The analysis of the bindingpatterns of Chitin synthetase to substrates, products and inhibitors at theatomic scale provides a stage for the realization of the dream ofenvironmentally friendly pesticides that has not been realized for decades byprecise design of green pesticide based on Chitin synthetase structure. Theconservation of the mechanism of Chitin synthesis in pests and diseases makesChitin synthetase important as a molecular target of green pesticides. Thisresearch achievement is a milestone, indicating that the level of pesticideresearch and development in China has risen to the height of originalinnovation of basic theory.

This work isalso one of the most important fundamental advances in global pesticideinnovation research and development in recent decades.

CAAS said thatthey will strengthen the application of the research results and speed up thedevelopment of green pesticides targeting the enzyme in the future.

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