Pigott Craig R, King Martin S, Ellar David J
Department of Biochemistry, University of Cambridge, 80 Tennis Court Road, Cambridge CB2 1GA, United Kingdom.
Appl Environ Microbiol. 2008 Jun;74(11):3497-511. doi: 10.1128/AEM.02844-07. Epub 2008 Apr 11.
Cry proteins are a large family of crystalline toxins produced by Bacillus thuringiensis. Individually, the family members are highly specific, but collectively, they target a diverse range of insects and nematodes. Domain II of the toxins is important for target specificity, and three loops at its apex have been studied extensively. There is considerable interest in determining whether modifications in this region may lead to toxins with novel specificity or potency. In this work, we studied the effect of loop substitution on toxin stability and specificity. For this purpose, sequences derived from antibody complementarity-determining regions (CDR) were used to replace native domain II apical loops to create "Crybodies." Each apical loop was substituted either individually or in combination with a library of third heavy-chain CDR (CDR-H3) sequences to create seven distinct Crybody types. An analysis of variants from each library indicated that the Cry1Aa framework can tolerate considerable sequence diversity at all loop positions but that some sequence combinations negatively affect structural stability and protease sensitivity. CDR-H3 substitution showed that loop position was an important determinant of insect toxicity: loop 2 was essential for activity, whereas the effects of substitutions at loop 1 and loop 3 were sequence dependent. Unexpectedly, differences in toxicity did not correlate with binding to cadherins--a major class of toxin receptors--since all Crybodies retained binding specificity. Collectively, these results serve to better define the role of the domain II apical loops as determinants of specificity and establish guidelines for their modification.
晶体蛋白是苏云金芽孢杆菌产生的一大类晶体毒素。该家族成员各自具有高度特异性,但总体上能靶向多种昆虫和线虫。毒素的结构域II对靶标特异性很重要,其顶端的三个环已得到广泛研究。人们对确定该区域的修饰是否会导致具有新特异性或效力的毒素有着浓厚兴趣。在这项研究中,我们研究了环替换对毒素稳定性和特异性的影响。为此,我们使用源自抗体互补决定区(CDR)的序列替换天然结构域II顶端环,以创建“晶体抗体”。每个顶端环单独替换,或与第三重链CDR(CDR-H3)序列库组合替换,从而创建了七种不同类型的晶体抗体。对每个文库变体的分析表明,Cry1Aa框架在所有环位置都能耐受相当大的序列多样性,但某些序列组合会对结构稳定性和蛋白酶敏感性产生负面影响。CDR-H3替换表明环位置是昆虫毒性的重要决定因素:环2对活性至关重要,而环1和环3替换的影响则取决于序列。出乎意料的是,毒性差异与与钙黏蛋白(一类主要的毒素受体)的结合无关,因为所有晶体抗体都保留了结合特异性。总体而言,这些结果有助于更好地界定结构域II顶端环作为特异性决定因素的作用,并为其修饰建立指导原则。