Wang Qi, Heizer Esley, Rosa Bruce A, Wildman Scott A, Janetka James W, Mitreva Makedonka
McDonnell Genome Institute, Washington University in St. Louis, St. Louis, MO, USA.
Carbone Cancer Center, School of Medicine and Public Health, University of Wisconsin, Madison, WI, USA.
Infect Genet Evol. 2016 Apr;39:201-211. doi: 10.1016/j.meegid.2016.01.025. Epub 2016 Jan 30.
Insertions and deletions (indels) are important sequence variants that are considered as phylogenetic markers that reflect evolutionary adaptations in different species. In an effort to systematically study indels specific to the phylum Nematoda and their structural impact on the proteins bearing them, we examined over 340,000 polypeptides from 21 nematode species spanning the phylum, compared them to non-nematodes and identified indels unique to nematode proteins in more than 3000 protein families. Examination of the amino acid composition revealed uneven usage of amino acids for insertions and deletions. The amino acid composition and cost, along with the secondary structure constitution of the indels, were analyzed in the context of their biological pathway associations. Species-specific indels could enable indel-based targeting for drug design in pathogens/parasites. Therefore, we screened the spatial locations of the indels in the parasite's protein 3D structures, determined the location of the indel and identified potential unique drug targeting sites. These indels could be confirmed by RNA-Seq data. Examples are presented illustrating the close proximity of some indels to established small-molecule binding pockets that can potentially facilitate selective targeting to the parasites and bypassing their host, thus reducing or eliminating the toxicity of the potential drugs. This study presents an approach for understanding the adaptation of pathogens/parasites at a molecular level, and outlines a strategy to identify such nematode-selective targets that remain essential to the organism. With further experimental characterization and validation, it opens a possible channel for the development of novel treatments with high target specificity, addressing both host toxicity and resistance concerns.
插入和缺失(indels)是重要的序列变异,被视为反映不同物种进化适应性的系统发育标记。为了系统地研究线虫门特有的插入和缺失及其对携带它们的蛋白质的结构影响,我们检查了来自该门21种线虫物种的超过340,000种多肽,将它们与非线虫物种进行比较,并在3000多个蛋白质家族中鉴定出线虫蛋白质特有的插入和缺失。对氨基酸组成的检查揭示了插入和缺失中氨基酸的使用不均衡。在其生物学途径关联的背景下,分析了插入和缺失的氨基酸组成、成本以及二级结构组成。物种特异性的插入和缺失可以使基于插入和缺失的靶向用于病原体/寄生虫的药物设计。因此,我们筛选了寄生虫蛋白质三维结构中插入和缺失的空间位置,确定了插入和缺失的位置,并确定了潜在的独特药物靶向位点。这些插入和缺失可以通过RNA测序数据得到证实。文中给出了一些例子,说明一些插入和缺失与已确定的小分子结合口袋非常接近,这有可能促进对寄生虫的选择性靶向并绕过其宿主,从而降低或消除潜在药物的毒性。本研究提出了一种在分子水平上理解病原体/寄生虫适应性的方法,并概述了一种识别对线虫至关重要的此类线虫选择性靶点的策略。通过进一步的实验表征和验证,它为开发具有高靶点特异性、解决宿主毒性和耐药性问题的新型治疗方法开辟了一条可能的途径。