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巨细胞病毒核心核出复合物(NEC)寡聚相互作用的特性及其对 NEC 抑制性小分子的敏感性。

Properties of Oligomeric Interaction of the Cytomegalovirus Core Nuclear Egress Complex (NEC) and Its Sensitivity to an NEC Inhibitory Small Molecule.

机构信息

Institute for Clinical and Molecular Virology, Friedrich-Alexander University of Erlangen-Nürnberg (FAU), 91054 Erlangen, Germany.

Department of Chemistry and Pharmacy, Division of Medicinal Chemistry, Friedrich-Alexander University of Erlangen-Nürnberg (FAU), Erlangen-Nürnberg, 91058 Erlangen, Germany.

出版信息

Viruses. 2021 Mar 11;13(3):462. doi: 10.3390/v13030462.

Abstract

Herpesviral nuclear egress is a regulated process shared by all family members, ensuring the efficient cytoplasmic release of viral capsids. In the case of human cytomegalovirus (HCMV), the core of the nuclear egress complex (NEC) consists of the pUL50-pUL53 heterodimer that builds hexameric lattices for capsid binding and multicomponent interaction, including NEC-associated host factors. A characteristic feature of NEC interaction is the N-terminal hook structure of pUL53 that binds to an alpha-helical groove of pUL50, thus termed as hook-into-groove interaction. This central regulatory element is essential for viral replication and shows structural-functional conservation, which has been postulated as a next-generation target of antiviral strategies. However, a solid validation of this concept has been missing. In the present study, we focused on the properties of oligomeric HCMV core NEC interaction and the antiviral activity of specifically targeted prototype inhibitors. Our data suggest the following: (i) transiently expressed, variably tagged versions of HCMV NEC proteins exert hook-into-groove complexes, putatively in oligomeric assemblies that are distinguishable from heterodimers, as shown by in vitro assembly and coimmunoprecipitation approaches; (ii) this postulated oligomeric binding pattern was further supported by the use of a pUL50::pUL53 fusion construct also showing a pronounced multi-interaction potency; (iii) using confocal imaging cellular NEC-associated proteins were found partly colocalized with the tagged core NECs; (iv) a small inhibitory molecule, recently identified by an in vitro binding inhibition assay, was likewise active in blocking pUL50-pUL53 oligomeric assembly and in exerting antiviral activity in HCMV-infected fibroblasts. In summary, the findings refine the previous concept of HCMV core NEC formation and nominate this drug-accessible complex as a validated antiviral drug target.

摘要

疱疹病毒核出芽是一种受调控的过程,所有家族成员都参与其中,以确保病毒衣壳在细胞质中的有效释放。在人类巨细胞病毒(HCMV)中,核出芽复合物(NEC)的核心由 pUL50-pUL53 异二聚体组成,该异二聚体构建六聚体晶格以结合衣壳并进行多成分相互作用,包括 NEC 相关的宿主因子。NEC 相互作用的一个特征是 pUL53 的 N 端钩结构与 pUL50 的α-螺旋槽结合,因此称为钩入槽相互作用。这个中央调节元件对于病毒复制是必不可少的,并且表现出结构功能的保守性,这被认为是下一代抗病毒策略的靶标。然而,这一概念的可靠验证一直缺失。在本研究中,我们专注于 HCMV 核心 NEC 相互作用的寡聚特性和针对特定靶标的原型抑制剂的抗病毒活性。我们的数据表明:(i)瞬时表达的、可变标记的 HCMV NEC 蛋白变体发挥钩入槽复合物,推测是在体外组装和共免疫沉淀方法中可区分的寡聚组装体;(ii)这种假定的寡聚结合模式进一步得到了 HCMV NEC 融合构建体的支持,该构建体也显示出明显的多相互作用能力;(iii)使用共聚焦成像,细胞内 NEC 相关蛋白被发现部分与标记的核心 NEC 共定位;(iv)一种最近通过体外结合抑制测定鉴定的小分子抑制剂,同样能够阻断 pUL50-pUL53 寡聚组装,并在 HCMV 感染的成纤维细胞中发挥抗病毒活性。总之,这些发现细化了之前的 HCMV 核心 NEC 形成概念,并将这个可接近药物的复合物指定为一个经过验证的抗病毒药物靶标。

https://cdn.ncbi.nlm.nih.gov/pmc/blobs/7786/8002134/50a172410aed/viruses-13-00462-g001.jpg

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