当前位置: Nature » 生物医学 » 正文


摘要 : 随着青蒿素耐药性越来越普遍,亟需开发以镰刀形疟原虫(疟疾的致病物)为目标的新治疗药物。在这项研究中,Ian Gilbert及同事报告了一种化合物(DDD107498)的发现,它对这种寄生虫生命周期多个阶段都具有抗疟疾活性.

 随着青蒿素耐药性越来越普遍,亟需开发以镰刀形疟原虫(疟疾的致病物)为目标的新治疗药物。在这项研究中,Ian Gilbert及同事报告了一种化合物(DDD107498)的发现,它对这种寄生虫生命周期多个阶段都具有抗疟疾活性,并且具有良好的药物动力特性和安全特性。它没有诱变性,同时既具有单剂量治疗的潜力、又具有每周一次的化学保护作用。DDD107498通过对细胞溶质蛋白合成的抑制发挥作用,以翻译伸长因子eEF2为其作用目标。


A novel multiple-stage antimalarial agent that inhibits protein synthesis


There is an urgent need for new drugs to treat malaria, with broad therapeutic potential and novel modes of action, to widen the scope of treatment and to overcome emerging drug resistance. Here we describe the discovery of DDD107498, a compound with a potent and novel spectrum of antimalarial activity against multiple life-cycle stages of the Plasmodium parasite, with good pharmacokinetic properties and an acceptable safety profile. DDD107498 demonstrates potential to address a variety of clinical needs, including single-dose treatment, transmission blocking and chemoprotection. DDD107498 was developed from a screening programme against blood-stage malaria parasites; its molecular target has been identified as translation elongation factor 2 (eEF2), which is responsible for the GTP-dependent translocation of the ribosome along messenger RNA, and is essential for protein synthesis. This discovery of eEF2 as a viable antimalarial drug target opens up new possibilities for drug discovery.

来源: Nature 浏览次数:0


RSS订阅 - 填写您的邮件地址,订阅我们的精彩内容: - 网站地图
网站联系电话:020-87540820 备案号:粤ICP备11050685号-8 增值电信业务经营许可证:粤B2-20120479
©2011-2015 生物帮 All rights reserved.