Leucyl-trna synthetase inhibitors for crop protection fungicide development
A series of novel Leucyl-tRNA synthetase (LeuRS) inhibitors with potent activity against major agricultural pathogens including Botrytis cinerea, Alternaria solani, and Gibberella zeae. Some compounds show inhibition rates of 100% at 50 μg/mL and over 95% at 1 μg/mL, outperforming existing fungicides like Boscalid and Carbendazim.
Overview
This research program focuses on developing novel Leucyl-tRNA synthetase (LeuRS) inhibitors as next-generation crop protection fungicides. LeuRS is an aminoacyl-tRNA synthetase that plays a critical role in protein synthesis and includes a proofreading editing domain (CP1) that ensures accurate tRNA aminoacylation. While LeuRS inhibitors have shown success in pharmaceutical applications (such as GSK3036656 for tuberculosis and Tavaborole for onychomycose), this work extends the approach to agricultural crop protection, where few LeuRS-targeted fungicides currently exist.
The lead compounds developed by the research team have demonstrated exceptional in vitro activity against major agricultural pathogens, including Botrytis cinerea (gray mold), Alternaria solani, Gibberella zeae (Fusarium graminearum), and Colletotrichum lagenarium. Several compounds achieved 100% inhibition rates at 50 μg/mL concentration against multiple pathogens, with some maintaining over 95% inhibition against Botrytis cinerea even at 1 μg/mL, outperforming commercial benchmarks such as Boscalid and Carbendazim.
Technical specifications
Core technology:
- Novel small-molecule inhibitors targeting the LeuRS editing domain (CP1)
- Compounds designed and synthesized with demonstrated in vitro antifungal activity
Key features:
- Broad-spectrum activity against key agricultural fungal pathogens
- High potency at low concentrations (over 95% inhibition at 1 μg/mL against Botrytis cinerea)
- Novel mechanism of action distinct from existing fungicides, potentially addressing resistance issues
- Activity superior to or comparable with commercial standards Boscalid and Carbendazim
Pathogens targeted:
- Botrytis cinerea (gray mold)
- Alternaria solani
- Gibberella zeae (Fusarium head blight)
- Colletotrichum lagenarium
- Alternaria leaf spot pathogens
Technology readiness level
The research is currently at the lead compound optimization stage. In vitro activity has been validated against multiple agricultural pathogens with promising results. Future work will focus on structural optimization of lead compounds to build a LeuRS inhibitor library for crop diseases, conducting safety, toxicity, and residue experiments on crops, and further refining molecular structures based on structure-activity and structure-toxicity relationships to identify candidate crop fungicide molecules ready for advanced development.
About Nanjing Agricultural University
Nanjing Agricultural University is a public research university with an agricultural focus in Nanjing, advancing national and regional priorities through integrated basic-to-applied research and field training. Industry engages through experimental farms, field stations, controlled-environment facilities, and pilot processing spaces for prototyping and scale‑up. An industry liaison team supports sponsored research, testing services, and joint labs, while regional demonstration sites speed on‑farm trials across the Yangtze River Delta. Research is supported by national and provincial programs, including the National Natural Science Foundation of China and the Ministry of Science and Technology. A technology transfer office manages IP, licensing, and startup incubation.
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