乙酰辅酶A羧化酶除草剂的抗性研究
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摘要
乙酰辅酶A羧化酶(Acetyl-CoA Carboxylase,简称ACCase)是植物代谢过程中催化植物脂肪酸合成的关键酶,是1958年发现的除草剂的一个作用靶标。ACCase类除草剂包括芳氧苯氧丙酸酯类(Aryloxyphenoxypropanoates,APP)、肟醚类环己二酮(Cyclohexanedione oximes,CHD)和苯基吡唑啉类(Phenylpyrazoline,DEN)三类~([1-2])。由于其选择性高,能够苗后防除一年或多年生禾本科杂草,且在植物体内传导,具有高效、低毒、施用期长、对后茬作物安全等优点,此类除草剂迅速发展、品种不断增多、使用面积迅速扩大,已成为世界第三类重要除草剂~([3])。然而随着其迅速大面积连续使用,杂草抗性相继发生且蔓延,根据HRAC(Herbicide Resistance Action Committee)统计,截止2015年,靶向ACCase的抗性杂草物种数目已然跃居第三位,因此研究ACCase除草剂的抗性机理显得尤为必要。基于此,本课题组对乙酰辅酶A的性质、羧基转移酶的晶体结构及其与除草剂分子盖草能(haloxyfop)的结合方式进行了研究,同时重点探讨了杂草对乙酰辅酶A羧化酶抑制剂产生抗性的原因,为合理药物分子设计提供了基础。
During the plant metabolic process,Acetyl-CoA Carboxylase(ACCase) is the key enzyme that catalyzes the synthesis of plant fatty acids.It is also the target of a herbicide found in 1958.Such herbicide targeting ACCase embraces three different categories,that is,Aryloxyphenoxypropanoates(APP),Cyclohexanedione oximes(CHD)and Phenylpyrazoline(DEN).But along with the long-term and big area use,the weed's resistance appeared quickly.This research group put emphasis on the crystal structure of Acetyl-CoA and Carboxylase,and their combination mode with haloxyfop,the herbicide molecule,discuss mainly on the reason for weed resistance to herbicide targeting ACCase,so as to provide reference to the design of reasonable drug molecule.
引文
[1]Huang,Tong-Hui;Zhu,Xiao-Lei;Zhang,Ai-Dong*;Tu,Hai-Yang.Eur.J.Med.Chem.2011,24,4588-4594.
    [2]Chao-Nan Chen,Qiong Chen,Yu-Chao Liu,Xiao-Lei Zhu,Cong-Wei Niu,Zhen Xi,*,Guang-Fu Yang.Bioorganic&Medicinal Chemistry 2010,18,4897-4904.
    [3]Zhang,G.F.;Zhu,X.L.;Miao,F.J.;Tian,D.M.;Li,H.B*.Org.Biomol.Chem.2012,10,3185-3188.

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