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激酶抑制剂 SFV785 将登革热病毒包膜蛋白从复制复合物中置换出来并阻断病毒组装。

The kinase inhibitor SFV785 dislocates dengue virus envelope protein from the replication complex and blocks virus assembly.

机构信息

Program in Emerging Infectious Diseases, Duke-NUS Graduate Medical School, Singapore.

出版信息

PLoS One. 2011;6(8):e23246. doi: 10.1371/journal.pone.0023246. Epub 2011 Aug 17.

Abstract

Dengue virus (DENV) is the etiologic agent for dengue fever, for which there is no approved vaccine or specific anti-viral drug. As a remedy for this, we explored the use of compounds that interfere with the action of required host factors and describe here the characterization of a kinase inhibitor (SFV785), which has selective effects on NTRK1 and MAPKAPK5 kinase activity, and anti-viral activity on Hepatitis C, DENV and yellow fever viruses. SFV785 inhibited DENV propagation without inhibiting DENV RNA synthesis or translation. The compound did not cause any changes in the cellular distribution of non-structural 3, a protein critical for DENV RNA synthesis, but altered the distribution of the structural envelope protein from a reticulate network to enlarged discrete vesicles, which altered the co-localization with the DENV replication complex. Ultrastructural electron microscopy analyses of DENV-infected SFV785-treated cells showed the presence of viral particles that were distinctly different from viable enveloped virions within enlarged ER cisternae. These viral particles were devoid of the dense nucleocapsid. The secretion of the viral particles was not inhibited by SFV785, however a reduction in the amount of secreted infectious virions, DENV RNA and capsid were observed. Collectively, these observations suggest that SFV785 inhibited the recruitment and assembly of the nucleocapsid in specific ER compartments during the DENV assembly process and hence the production of infectious DENV. SFV785 and derivative compounds could be useful biochemical probes to explore the DENV lifecycle and could also represent a new class of anti-virals.

摘要

登革热病毒(DENV)是登革热的病原体,目前尚无批准的疫苗或特定的抗病毒药物。作为对此的补救措施,我们探索了使用干扰必需宿主因子作用的化合物,并在这里描述了一种激酶抑制剂(SFV785)的特性,该抑制剂对 NTRK1 和 MAPKAPK5 激酶活性具有选择性作用,并且对丙型肝炎、登革热和黄热病病毒具有抗病毒活性。SFV785 抑制 DENV 增殖而不抑制 DENV RNA 合成或翻译。该化合物不会引起非结构 3 的细胞分布发生任何变化,非结构 3 蛋白对于 DENV RNA 合成至关重要,但改变了结构包膜蛋白的分布,从网状网络变为扩大的离散囊泡,从而改变了与 DENV 复制复合物的共定位。感染 DENV 的 SFV785 处理细胞的超微结构电子显微镜分析显示,存在明显不同于内质网腔中扩大的 ER 中存在的有活力包膜病毒的病毒颗粒。这些病毒颗粒没有致密的核衣壳。SFV785 并未抑制病毒颗粒的分泌,但是观察到分泌的传染性病毒颗粒、DENV RNA 和衣壳的量减少。总的来说,这些观察结果表明,SFV785 抑制了核衣壳在 DENV 组装过程中在特定 ER 隔室中的募集和组装,因此产生了传染性 DENV。SFV785 和衍生化合物可以用作探索 DENV 生命周期的有用生化探针,并且也可以代表一类新的抗病毒药物。

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