伯豪生物转化医学服务平台
威斯腾促销
贝康招聘

新药物标靶“休眠” 疟原虫

2011/11/18 来源:Eurekalert
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导读
研究人员已经发现了一系列的化合物。这些化合物显示,它们有希望在疟原虫进入血流之前在肝脏中孵化的时候将其杀灭。

研究人员已经发现了一系列的化合物。这些化合物显示,它们有希望在疟原虫进入血流之前在肝脏中孵化的时候将其杀灭。人们急需这样的药物来治疗间日疟原虫,这是在非洲以外地区的主要的疟原虫种类。

间日疟原虫与致命的恶性虐原虫不同,因为它会在肝脏中进入一种“休眠期”,这时该疟原虫被称作是一种休眠子。休眠子可在感染的蚊子叮咬了其宿主之后数月甚或数年时重新出现在血液之中。

间日疟原虫感染的慢性和长时间持续的性质对感染者的健康和经济状况都会产生重大的影响。Stephan Meister及其同事应用一种自动化显微镜检测方法来筛检成千上万种已知可杀灭血液期疟原虫的化合物,希望能够找到那些也能杀灭肝脏期疟原虫的化合物。

他们发现了一系列的叫做咪唑嗪的可以口服并能阻止在小鼠模型中疟原虫在肝细胞内发育的化合物。(生物探索)

相关英文论文摘要:

Imaging of Plasmodium Liver Stages to Drive Next-Generation Antimalarial Drug Discovery

Most malaria drug development focuses on parasite stages detected in red blood cells, even though to achieve eradication, next-generation drugs active against both erythrocytic and exo-erythrocytic forms would be preferable. We applied a multifactorial approach to a set of >4,000 commercially available compounds with previously demonstrated blood stage activity (IC50 < 1 µM), and identified chemical scaffolds with potent activity against both forms. From this screen, we identified an imidazolopiperazine scaffold series that was highly enriched among compounds active against Plasmodium liver stages. Our orally bioavailable lead imidazolopiperazine confers complete causal prophylactic protection (15 mg/kg) in rodent models of malaria and shows potent in vivo blood-stage therapeutic activity. The open source chemical tools resulting from our effort provide starting points for future drug discovery programs, as well as opportunities for researchers to investigate the biology of exo-erythrocytic forms.

英文论文链接: http://www.sciencemag.org/content/early/2011/11/16/science.1211936

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