中文摘要
农药分子靶标创新是农药创新的关键科学问题。申请人针对昆虫蜕皮中独特的表皮几丁质降解与合成,以农业害虫亚洲玉米螟为对象,①发现表皮几丁质降解与合成同工酶家族谱;②发现OfHex1和OfChtI分别是关键的降解外切酶和内切酶,并阐明其协同性、晶体结构及其迥异于人酶的显著结构差异性等科学问题;③针对结构差异设计并发现3个能导致玉米螟蜕皮不正常而死亡的小分子酶抑制剂。成果为农药创新提供了具有潜力的新分子靶标,引起日本、法国等本领域著名学者关注和应用。近5年在Acta Cryst D (IF14.1)、JBC(IF4.6)、BJ(IF4.6)、IBMB(IF3.2)、IMB(IF3.0)等期刊发表通讯作者论文31篇,申请专利5项。任2个国际期刊编委,荷兰科学研究基金会NWO项目评审专家,主编Current Drug Targets农药靶标专辑。曾获教育部新世纪人才、辽宁省百人计划及霍英东青年基金。
英文摘要
Innovation of pesticide molecular targets is the key scientific issue for the development of novel pesticides. Focusing on cuticular chitin degradation and synthesis, the most vital bioprocess during insect molting, this applicant has worked on the most destructive pest, Ostrinia furnacalis. The main achievements this applicant has made, include: 1) the discovery of a series of enzyme homologs associated with chitinolytic and chitin synthestic processes; 2) the identification of two key enzymes,the exo-acting chitinolytic enzyme OfHex1 and the endo-acting chitinolytic enzyme OfChtI, and their synergistic manner during chitin degradation as well as disctinct structural features from human enzyme homologs; 3) the obtainment of structural-based designed, highly efficient and insect-specific small molecule inhibitors against the two enzymes. These achievements provide promising target potentials for developing novel pesticides, and have been cited and highlighted by world-wide researchers such as those from Japan, France and Czech. In the last five years, as a corresponding author, the applicant has published 31 research papers in SCI journals including Acta Crystallogr. D (IF14.1)、JBC(IF4.6)、BJ(IF4.6)、IBMB(IF3.2)、IMB(IF3.0) as well. The applicant has applied 5 Chinese invention patents. This applicant also acts as editorial board members of two international journals and has been invited to be a guest editor to organize a hot topic issue of the journal Current Drug Targets. As a specialist in insect chitinolytic enzymes, this applicant has been invited to review research proposals submitted to the Netherlands Organisation for Scientific Research (NWO), the most prominent financier of science in the Netherlands. The hornors and awards this applicant has obtained include “New Century Excellent Talents in Universities” sponsored by Chinese Ministry of Education, Fok Ying Tung Fund for Young Research sponsored by Chinese Ministry of Education and “Bai-Qian-Wan Intelligence ” sponsored by Education Department ofLiaoning Province.
