Yadav Sunita, Gupta Smita, Saxena Jitendra Kumar
Division of Biochemistry, CSIR-Central Drug Research Institute, BS10/1, Sector 10, Jankipuram extension, Sitapur Road, Lucknow 226021, Uttar Pradesh, India.
Division of Biochemistry, CSIR-Central Drug Research Institute, BS10/1, Sector 10, Jankipuram extension, Sitapur Road, Lucknow 226021, Uttar Pradesh, India.
Int J Biol Macromol. 2017 Sep;102:986-995. doi: 10.1016/j.ijbiomac.2017.04.053. Epub 2017 Apr 14.
Calreticulin of Brugia malayi (BmCRT) play very important role in host-parasite interaction. In previous study it was found that BmCRT is responsible for prevention of host classical complement pathway activation via its interaction with first component C1q of the human host. Therefore, BmCRT is an essential protein for parasite survival and an important drug target to fend filariasis. In the present study, we have carried out a systamatic biophysical characterization of BmCRT protein. Unfolding of BmCRT was found to be non-cooperative two-state process in the presence of both denaturant GdmCl and urea. The results also illustrated that protein lost its 50% activity at 1.5M GdmCl and 3M Urea. Partially unfolded and molten-globule like intermediate state was observed at 0.8 to 1.2M GdmCl while Urea unfolding showed intermediate state at 1.2 to 1.6M. Unfolding pathway monitored with the help of apolar quencher, favor above observations. All of these findings support the presence of detectable intermediate state during unfolding pathway of BmCRT. Furthermore, this study indicates that BmCRT is more stable toward temperature (Tm=65°C), pH and trypsin digestion. These differences in properties as compared to host can be fruitfully utilized for synthesis of compounds effective against the parasite.
马来布鲁线虫的钙网蛋白(BmCRT)在宿主与寄生虫的相互作用中起着非常重要的作用。在先前的研究中发现,BmCRT通过与人宿主的第一成分C1q相互作用,负责阻止宿主经典补体途径的激活。因此,BmCRT是寄生虫生存所必需的蛋白质,也是防治丝虫病的重要药物靶点。在本研究中,我们对BmCRT蛋白进行了系统的生物物理表征。发现在变性剂盐酸胍(GdmCl)和尿素存在的情况下,BmCRT的去折叠是一个非协同的两态过程。结果还表明,该蛋白在1.5M GdmCl和3M尿素时失去了50%的活性。在0.8至1.2M GdmCl时观察到部分去折叠和类似熔球的中间状态,而尿素去折叠在1.2至1.6M时显示中间状态。借助非极性猝灭剂监测的去折叠途径支持上述观察结果。所有这些发现都支持在BmCRT的去折叠途径中存在可检测的中间状态。此外,本研究表明BmCRT对温度(Tm=65°C)、pH和胰蛋白酶消化更稳定。与宿主相比,这些性质上的差异可有效地用于合成对寄生虫有效的化合物。