Super short membrane-active lipopeptides inhibiting the entry of influenza A virus

被引：17

作者：

Wu, Wenjiao ^{[1
]}

Wang, Jingyu ^{[1
]}

Lin, Dongguo ^{[1
]}

Chen, Linqing ^{[1
]}

Xie, Xiangkun ^{[1
]}

Shen, Xintian ^{[1
]}

Yang, Qingqing ^{[1
]}

Wu, Qiuyi ^{[1
]}

Yang, Jie ^{[1
]}

He, Jian ^{[1
]}

Liu, Shuwen ^{[1
]}

机构：

[1] Southern Med Univ, Sch Pharmaceut Sci, Guangzhou 510515, Guangdong, Peoples R China

来源：

BIOCHIMICA ET BIOPHYSICA ACTA-BIOMEMBRANES | 2015年 / 1848卷 / 10期

基金：

中国国家自然科学基金;

关键词：

Influenza A virus; Virus entry inhibitor; Short lipopeptide; Membrane fusion; Fusion inhibition; Virus-cell fusion; TIME RT-PCR; RECEPTOR-BINDING; ANTIINFLUENZA VIRUS; NEURAMINIDASE; INFECTION; HOST; HEMAGGLUTININ; REPLICATION; OSELTAMIVIR; FUSION;

D O I：

10.1016/j.bbamem.2015.06.015

中图分类号：

Q5 [生物化学]; Q7 [分子生物学];

学科分类号：

071010 ; 081704 ;

摘要：

Influenza A viruses (IAV) are significant pathogens that result in millions of human infections and impose a substantial health and economic burdens worldwide. Due to the limited anti-influenza A therapeutics available and the emergence of drug resistant viral strains, it is imperative to develop potent anti-IAV agents with different mode of action. In this study, by applying a pseudovirus based screening approach, two super short membrane-active lipopeptides of C12-KKWK and C12-OOWO were identified as effective anti-IAV agents with IC50 value of 7.30 +/- 1.57 and 8.48 +/- 0.74 mg/L against A/Puerto Rico/8/34 strain, and 6.14 +/- 1.45 and 7.22 +/- 0.67 mg/L against A/Aichi/2/68 strain, respectively. The mechanism study indicated that the anti-IAV activity of these peptides would result from the inhibition of virus entry by interacting with HA2 subunit of hemagglutinin (HA). Thus, these peptides may have potentials as lead peptides for the development of new anti-IAV therapeutics to block the entry of virus into host cells. (c) 2015 Elsevier B.V. All rights reserved.

引用

页码：2344 / 2350

页数：7

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