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首页 > 医学词汇大全 > oseltamivir phosphate
oseltamivir phosphate

呼吸

关键词呼吸 药物 流感治疗药物

词汇介绍

拓展阅读

解析

oseltamivir   /'ozltəmɪvɚ/

       n. 奥司他韦

       All other viruses have been shown sensitive to both oseltamivir and zanamivir.所有其它病毒显示对奥司他韦和扎那米韦都是敏感的。

 

phosphate   /'fɑsfet/ 

       n. 磷酸盐

同根词   phosphatase n. [生化] 磷酸酶

               phosphocreatine n. [生化] 磷酸肌酸(等于phosphocreatin)

       Each consists of a nucleoside and one or more phosphate groups. 每个核酸都由一个核和一个或多个磷酸盐基团组成。

概述

基本信息药物达菲(磷酸奥司他韦胶囊)主要成份为磷酸奥司他韦。化学式:(3R,4R,5S)-4-乙酰氨基-5-氨基-3(1-乙丙氧基)-1-环乙烯-1羧酸乙酯磷酸盐。分子式:C16H28N2O4·H3PO4。分子量:410.40。 作用机制磷酸奥司他韦是奥司他韦活性代谢产物的药物前体,奥司他韦的活性代谢产物是强效的选择性流感病毒神经氨酸酶抑制剂。病毒神经氨酸酶活性对新形成的病毒颗粒从被感染细胞的释放和感染性病毒在人体内进一步传播是关键的。奥司他韦的活性代谢产物抑制A型和B型流感病毒的神经

An Influenza Virus Entry Inhibitor Targets Class II PI3 Kinase and Synergizes with Oseltamivir.复制标题

一种流感病毒进入抑制剂靶向II类PI3激酶并与奥司他韦协同作用。

发表时间:2019-09-09

影响因子:4.9

作者: O'Hanlon R

期刊:ACS Infect Dis

Two classes of antivirals targeting the viral neuraminidase (NA) and endonuclease are currently the only clinically useful drugs for the treatment of influenza. However, resistance to both antivirals has been observed in clinical isolates, and there was widespread resistance to oseltamivir (an NA inhibitor) among H1N1 viruses prior to 2009. This potential for resistance and lack of diversity for antiviral targets highlights the need for new influenza antivirals with a higher barrier to resistance. In this study, we identified an antiviral compound, M85, that targets host kinases, epidermal growth factor receptor (EGFR), and phosphoinositide 3 class II β (PIK3C2β) and is not susceptible to resistance by viral mutations. M85 blocks endocytosis of influenza viruses and inhibits a broad-spectrum of viruses with minimal cytotoxicity. In vitro, we found that combinations of M85 and oseltamivir have strong synergism. In the mouse model for influenza, treatment with the combination therapy was more protective against a lethal viral challenge than oseltamivir alone, indicating that development of M85 could lead to combination therapies for influenza. Finally, through this discovery of M85 and its antiviral mechanism, we present the first description of PIK3C2β as a necessary host factor for influenza virus entry.

译文

靶向病毒神经氨酸酶(NA)和内切核酸酶的两类抗病毒药物是目前唯一用于治疗流感的临床有用药物。然而,在临床分离株中已经观察到对两种抗病毒药物的抗性,并且在2009年之前对H1N1病毒中的奥司他韦(一种NA抑制剂)具有广泛的抗性。抗病毒靶标的抗性和缺乏多样性的潜力强调了对新型流感抗病毒药物的需求。具有更高的抵抗力障碍。在这项研究中,我们确定了一种抗病毒化合物M85,其靶向宿主激酶,表皮生长因子受体(EGFR)和磷酸肌醇3类IIβ(PIK3C2β),并且不易受病毒突变的抵抗。 M85阻断流感病毒的内吞作用并抑制广谱病毒,并具有最小的细胞毒性。在体外,我们发现M85和奥司他韦的组合具有强烈的协同作用。在用于流感的小鼠模型中,与单独的奥司他韦相比,使用联合疗法的治疗对致死性病毒攻击更具保护作用,表明M85的发展可导致针对流感的组合疗法。最后,通过M85及其抗病毒机制的这一发现,我们首次将PIK3C2β描述为流感病毒进入的必需宿主因子。