Kelleher Alan, Zhan Bin, Asojo Oluwatoyin A
Department of Pediatrics, Baylor College of Medicine, 1102 Bates Avenue BCM 320, Houston, TX 77030, USA.
Acta Crystallogr Sect F Struct Biol Cryst Commun. 2013 Aug;69(Pt 8):839-43. doi: 10.1107/S1744309113017661. Epub 2013 Jul 27.
Necator americanus is the major cause of human hookworm infection, which is a global cause of anemia in the developing world. Ongoing efforts to control hookworm infection include the identification of candidate vaccine antigens as well as potential therapeutic targets from the infective L3 larval stages and adult stages of the parasite. One promising family of proteins are the adult-stage-secreted cytosolic glutathione S-transferases (GSTs). Nematode GSTs facilitate the inactivation and degradation of a variety of electrophilic substrates (drugs) via the nucleophilic addition of reduced glutathione. Parasite GSTs also play significant roles in multi-drug resistance and the modulation of host immune defense mechanisms. Here, the structure of Na-GST-3, one of three GSTs secreted by adult-stage N. americanus, is reported. Unlike most GST structures, the Na-GST-3 crystal contains a monomer in the asymmetric unit. However, the monomer forms a prototypical GST dimer across the crystallographic twofold. A glutathione from the fermentation process is bound to the monomer. The overall binding cavity of Na-GST-3 is reminiscent of that of other N. americanus GSTs and is larger and capable of binding a wider array of ligands than GSTs from organisms that have other major detoxifying mechanisms. Furthermore, despite having low sequence identity to the host GST, Na-GST-3 has a greater tertiary-structure similarity to human sigma-class GST than was observed for the other N. americanus GSTs.
美洲板口线虫是人类钩虫感染的主要病因,在发展中世界,它是导致贫血的一个全球性因素。目前控制钩虫感染的努力包括从寄生虫的感染性L3幼虫阶段和成虫阶段识别候选疫苗抗原以及潜在的治疗靶点。一类有前景的蛋白质是成虫阶段分泌的胞质谷胱甘肽S-转移酶(GSTs)。线虫GSTs通过还原型谷胱甘肽的亲核加成促进多种亲电底物(药物)的失活和降解。寄生虫GSTs在多药耐药性以及宿主免疫防御机制的调节中也发挥着重要作用。在此,报道了美洲板口线虫成虫分泌的三种GSTs之一的Na-GST-3的结构。与大多数GST结构不同,Na-GST-3晶体在不对称单元中包含一个单体。然而,该单体在晶体学二重轴上形成一个典型的GST二聚体。来自发酵过程的一个谷胱甘肽与单体结合。Na-GST-3的整体结合腔让人联想到其他美洲板口线虫GSTs的结合腔,并且比具有其他主要解毒机制的生物体的GSTs更大,能够结合更广泛的配体。此外,尽管与宿主GST的序列同一性较低,但与其他美洲板口线虫GSTs相比,Na-GST-3与人类sigma类GST具有更高的三级结构相似性。