选择性靶向磷酸二酯酶，开发强效抗寄生虫药物。

IF 7 1区医学 Q1 PARASITOLOGY

Trends in parasitology Pub Date : 2024-11-15 DOI:10.1016/j.pt.2024.11.001

Shahbaz M Khan, Md Mukthar Mia, William H Witola

引用次数: 0

摘要

细胞内环核苷酸的调节是通过磷酸二酯酶（PDEs）的分解活动来实现的，以避免体内平衡失调。最近，Ajiboye 等人报告了将隐孢子虫 PDE1（CpPDE1）作为可行药物靶点的验证结果，并确定了优化的吡唑嘧啶类药物，它们对 CpPDE1 的选择性活性优于人类 PDEs，并具有强大的抗隐孢子虫功效。

本文章由计算机程序翻译，如有差异，请以英文原文为准。

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Selective targeting of phosphodiesterases to develop potent antiparasitic drugs.

Regulation of intracellular cyclic nucleotides to avoid homeostatic imbalances is achieved through catabolic activity of phosphodiesterases (PDEs). Recently, Ajiboye et al. reported validation of Cryptosporidium PDE1 (CpPDE1) as a viable drug target and identified optimized pyrazolopyrimidines with selective activity against CpPDE1 over human PDEs and with potent anticryptosporidial efficacy.

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来源期刊

Trends in parasitology 医学-寄生虫学

CiteScore

14.00

自引率

3.10%

发文量

148

审稿时长

6-12 weeks

期刊介绍： Since its inception as Parasitology Today in 1985, Trends in Parasitology has evolved into a highly esteemed review journal of global significance, reflecting the importance of medical and veterinary parasites worldwide. The journal serves as a hub for communication among researchers across all disciplines of parasitology, encompassing endoparasites, ectoparasites, transmission vectors, and susceptible hosts. Each monthly issue of Trends in Parasitology offers authoritative, cutting-edge, and yet accessible review articles, providing a balanced and comprehensive overview, along with opinion pieces offering personal and novel perspectives. Additionally, the journal publishes a variety of short articles designed to inform and stimulate thoughts in a lively and widely-accessible manner. These include Science & Society (discussing the interface between parasitology and the general public), Spotlight (highlighting recently published research articles), Forum (presenting single-point hypotheses), Parasite/Vector of the Month (featuring a modular display of the selected species), Letter (providing responses to recent articles in Trends in Parasitology), and Trendstalk (conducting interviews). Please note that the journal exclusively publishes literature reviews based on published data, with systematic reviews, meta-analysis, and unpublished primary research falling outside our scope.