Laboratory for Structural Biology of Infection and Inflammation, University of Hamburg, c/o DESY, Building 22a, Notkestrasse 85, 22607 Hamburg, Germany.
Institut für Zoophysiologie, Westfälische Wilhelms-Universität Münster, Schlossplatz 8, 48143 Münster, Germany.
Acta Crystallogr F Struct Biol Commun. 2022 Jun 1;78(Pt 6):232-240. doi: 10.1107/S2053230X22005350. Epub 2022 May 27.
Superoxide dismutases (SODs) are metalloproteins that are responsible for the dismutation of superoxide anion radicals. SODs are consequently protective against oxidative damage to cellular components. Among other protective mechanisms, the filarial parasite Onchocerca volvulus has a well developed defense system to scavenge toxic free radicals using SODs during migration and sojourning of the microfilariae and adult worms in the human body. O. volvulus is responsible for the neglected disease onchocerciasis or `river blindness'. In the present study, an extracellular Cu/Zn-SOD from O. volvulus (OvEC-SOD) was cloned, purified and crystallized to obtain structural insight into an attractive drug target with the potential to combat onchocerciasis. The recombinant OvEC-SOD forms a dimer and the protein structure was solved and refined to 1.55 Å resolution by X-ray crystallography. Interestingly, a sulfate ion supports the coordination of the conserved copper ion. The overall protein shape was verified by small-angle X-ray scattering. The enzyme shows a different surface charge distribution and different termini when compared with the homologous human SOD. A distinct hydrophobic cleft to which both protomers of the dimer contribute was utilized for a docking approach with compounds that have previously been identified as SOD inhibitors to highlight the potential for individual structure-based drug development.
超氧化物歧化酶(SODs)是一类金属蛋白酶,可促使超氧阴离子自由基发生歧化反应。因此,SOD 能够保护细胞成分免受氧化损伤。在其他保护机制中,丝虫寄生虫旋毛虫具有发达的防御系统,可利用 SOD 清除迁移和滞留在人体中的微丝蚴和成虫中的有毒自由基。旋毛虫是导致被忽视疾病盘尾丝虫病(“河盲症”)的罪魁祸首。在本研究中,从旋毛虫中克隆、纯化并结晶了一种细胞外 Cu/Zn-SOD(OvEC-SOD),以深入了解具有对抗盘尾丝虫病潜力的有吸引力的药物靶标。重组 OvEC-SOD 形成二聚体,通过 X 射线晶体学解析并将蛋白质结构精细解析至 1.55 Å 分辨率。有趣的是,一个硫酸根离子支持保守铜离子的配位。与同源的人 SOD 相比,整个蛋白质形状通过小角度 X 射线散射得到验证。与先前被鉴定为 SOD 抑制剂的化合物进行对接研究时,该酶表现出不同的表面电荷分布和不同的末端,这突出了基于单个结构的药物开发的潜力。