首页> 外文会议>European Symposium on Organic Chemistry >Acyclic nucleoside phosphonates as a new class of anti-malarial compounds: Inhibition of Plasmodium falciparum hypoxanthine-guahine-xanthine phosphoribosyltransferase by 9-2-(2-phosphonoethoxy)ethyl-purines and their branched derivatives
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Acyclic nucleoside phosphonates as a new class of anti-malarial compounds: Inhibition of Plasmodium falciparum hypoxanthine-guahine-xanthine phosphoribosyltransferase by 9-2-(2-phosphonoethoxy)ethyl-purines and their branched derivatives

机译:环状核苷膦酸盐作为一种新的抗疟疾化合物:抑制疟原虫脱氧黄嘌呤 - 黄嘌呤 - 黄嘌呤磷酰基转移酶的抑制作用9- 2-(2-膦酰基乙氧基)乙基 - 杂物和其支化衍生物

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摘要

The majority of lethal cases of malaria are caused by Plasmodium falciparum (Pf). These protozoan parasites can only produce purine nucleotides from the bases obtained from their host, while mammals are able to synthesize purine derivatives de novo as well as by salvage of preformed bases. Hypoxanthine-guanine-xanthine phosphoribosyltransferase (HGXPRT) is the key enzyme of purine salvage pathway, its activity has been shown to be essential for the survival of the parasite and so it represents a suitable drug target.
机译:大多数疟疾病例的疟疾病例是由疟原虫(PF)引起的。这些原生动物寄生虫只能从其宿主获得的碱中产生嘌呤核苷酸,而哺乳动物能够合成嘌呤衍生物DE NOVO以及通过预成型碱的挽救。缺氧 - 鸟嘌呤 - 黄嘌呤磷纤维基转移酶(HGXPRT)是嘌呤救生途径的关键酶,其活性已显示对寄生虫的存活至关重要,因此它代表了合适的药物靶标。

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