Department of Molecular Tropical Medicine and Genetics, Faculty of Tropical Medicine, Mahidol University, Bangkok, Thailand.
Department of Helminthology, Faculty of Tropical Medicine, Mahidol University, Bangkok, Thailand.
Sci Rep. 2024 Jun 5;14(1):12969. doi: 10.1038/s41598-024-63869-0.
Schistosomiasis, caused by Schistosoma trematodes, is a significant global health concern, particularly affecting millions in Africa and Southeast Asia. Despite efforts to combat it, the rise of praziquantel (PZQ) resistance underscores the need for new treatment options. Protein kinases (PKs) are vital in cellular signaling and offer potential as drug targets. This study focused on focal adhesion kinase (FAK) as a candidate for anti-schistosomal therapy. Transcriptomic and proteomic analyses of adult S. mekongi worms identified FAK as a promising target due to its upregulation and essential role in cellular processes. Molecular docking simulations assessed the binding energy of FAK inhibitors to Schistosoma FAK versus human FAK. FAK inhibitor 14 and PF-03814735 exhibited strong binding to Schistosoma FAK with minimal binding for human FAK. In vitro assays confirmed significant anti-parasitic activity against S. mekongi, S. mansoni, and S. japonicum, comparable to PZQ, with low toxicity in human cells, indicating potential safety. These findings highlight FAK as a promising target for novel anti-schistosomal therapies. However, further research, including in vivo studies, is necessary to validate efficacy and safety before clinical use. This study offers a hopeful strategy to combat schistosomiasis and reduce its global impact.
血吸虫病是由血吸虫引起的,是一个严重的全球健康问题,尤其在非洲和东南亚地区,影响了数百万人。尽管已经做出了努力来对抗这种疾病,但吡喹酮(PZQ)耐药性的出现凸显了需要新的治疗选择。蛋白激酶(PKs)在细胞信号转导中至关重要,是潜在的药物靶点。本研究集中于粘着斑激酶(FAK)作为抗血吸虫治疗的候选药物。对成年湄公血吸虫的转录组和蛋白质组分析表明,由于其上调和在细胞过程中的重要作用,FAK 是一个很有前途的靶点。分子对接模拟评估了 FAK 抑制剂与血吸虫 FAK 与人类 FAK 的结合能。FAK 抑制剂 14 和 PF-03814735 与 Schistosoma FAK 具有很强的结合能力,而与人类 FAK 的结合能力很小。体外实验证实了对湄公血吸虫、曼氏血吸虫和日本血吸虫的显著抗寄生虫活性,与 PZQ 相当,对人细胞的毒性较低,表明有潜在的安全性。这些发现突出了 FAK 作为一种有前途的抗血吸虫治疗新靶点。然而,在临床应用之前,还需要进一步的研究,包括体内研究,以验证疗效和安全性。本研究为抗击血吸虫病和降低其全球影响提供了一个有希望的策略。