Fournier D
IPBS, Biotechnologie des Proteines, 205 route de Narbonne, 31077 Toulouse, France.
Chem Biol Interact. 2005 Dec 15;157-158:257-61. doi: 10.1016/j.cbi.2005.10.040. Epub 2005 Nov 7.
Resistance-modified acetylcholinesterases have been described in many insect species and sequencing of their genes has allowed several point mutations to be described. Most mutations line the active site gorge. Each mutation provides a specific resistance pattern: it confers resistance to one insecticide but may increase sensitivity to another. Most mutations alter hydrolysis of the substrate by decreasing the rate of enzyme deacetylation and by diminishing the stability of the enzyme. Mutations are often found in combination in the same protein. This has several consequences: it increases the level of resistance, it enlarges the spectrum of resistance and it may restore the catalytic efficiency of the enzyme. Natural populations are heterogeneous, composed of a mixture of different alleles.
在许多昆虫物种中都已发现了抗性修饰的乙酰胆碱酯酶,对其基因进行测序后已描述了多个点突变。大多数突变位于活性位点峡谷周围。每个突变都呈现出特定的抗性模式:它赋予对一种杀虫剂的抗性,但可能会增加对另一种杀虫剂的敏感性。大多数突变通过降低酶的脱乙酰化速率和降低酶的稳定性来改变底物的水解。突变常常在同一蛋白质中组合出现。这会产生多种后果:它会提高抗性水平、扩大抗性谱,并且可能恢复酶的催化效率。自然种群是异质的,由不同等位基因的混合物组成。