Recombinant protein of heptad-repeat HR212, a stable fusion inhibitor with potent anti-HIV action in vitro

	Recombinant protein of heptad-repeat HR212, a stable fusion inhibitor with potent anti-HIV action in vitro
	Pang W 1,2,3; Wang RR 2; Yang LM 2; Liu CM 1; Tien P1; Zheng YT2; tienpo@sun.im.ac.cn ; zhengyt@mail.kiz.ac.cn
	2008
发表期刊	Virology
卷号	377 期号:1 页码:80-87
合作性质	其它
摘要	HR212, a recombinant protein expressed in Escherichia coli, has been previously reported to inhibit HIV-1 membrane fusion at low nanomolar level. Here we report that HR212 is effective in blocking laboratory strain HIV-1,B entry and replication with EC50 values of 3.92 +/- 0.62 and 6.59 +/- 1.74 nM, respectively, and inhibiting infection by clinic isolate HIV-1(KM018)with EC50 values of 44.44 +/- 10.20 nM, as well as suppressing HIV-1-induced cytopathic effect with an EC50 value of 3.04 +/- 1.20 nM. It also inhibited HIV-2(ROD) and HIV-2(CBL-20) entry and replication in the mu M range. Notably, HR212 was highly effective against T20-resistant strains with EC50 values ranging from 5.09 to 7.75 nM. Unlike T20, HR212 showed stability sufficient to inhibit syncytia formation in a time-of-addition assay, and was insensitive to proteinase K digestion These results suggest that HR212 has great potential to be further developed as novel HIV-1 fusion inhibitor for treatment of HIV/AIDS patients, particularly for those infected by T20-resistant variants.
关键词	Anti-hiv Agents Proteinase k T20-resistant Strains Hr212 Enfuvirtide Fusion Inhibitor Hiv-1 Hiv-2
资助者	This work was supported in part by grants from 863 Program (2006AA02A241) and the Outstanding Overseas Chinese Scholars Fund of the CAS for IMCAS, and from the CAS Program (KSCX1-YW-R-15, KSCX1-YW-R-24), 973 Program (2006CB504208, 2006CB504302), and Key Technological R&D Program of Yunnan (2004NG12) ; This work was supported in part by grants from 863 Program (2006AA02A241) and the Outstanding Overseas Chinese Scholars Fund of the CAS for IMCAS, and from the CAS Program (KSCX1-YW-R-15, KSCX1-YW-R-24), 973 Program (2006CB504208, 2006CB504302), and Key Technological R&D Program of Yunnan (2004NG12) ; This work was supported in part by grants from 863 Program (2006AA02A241) and the Outstanding Overseas Chinese Scholars Fund of the CAS for IMCAS, and from the CAS Program (KSCX1-YW-R-15, KSCX1-YW-R-24), 973 Program (2006CB504208, 2006CB504302), and Key Technological R&D Program of Yunnan (2004NG12) ; This work was supported in part by grants from 863 Program (2006AA02A241) and the Outstanding Overseas Chinese Scholars Fund of the CAS for IMCAS, and from the CAS Program (KSCX1-YW-R-15, KSCX1-YW-R-24), 973 Program (2006CB504208, 2006CB504302), and Key Technological R&D Program of Yunnan (2004NG12)
收录类别	SCI
语种	英语
资助者	This work was supported in part by grants from 863 Program (2006AA02A241) and the Outstanding Overseas Chinese Scholars Fund of the CAS for IMCAS, and from the CAS Program (KSCX1-YW-R-15, KSCX1-YW-R-24), 973 Program (2006CB504208, 2006CB504302), and Key Technological R&D Program of Yunnan (2004NG12) ; This work was supported in part by grants from 863 Program (2006AA02A241) and the Outstanding Overseas Chinese Scholars Fund of the CAS for IMCAS, and from the CAS Program (KSCX1-YW-R-15, KSCX1-YW-R-24), 973 Program (2006CB504208, 2006CB504302), and Key Technological R&D Program of Yunnan (2004NG12) ; This work was supported in part by grants from 863 Program (2006AA02A241) and the Outstanding Overseas Chinese Scholars Fund of the CAS for IMCAS, and from the CAS Program (KSCX1-YW-R-15, KSCX1-YW-R-24), 973 Program (2006CB504208, 2006CB504302), and Key Technological R&D Program of Yunnan (2004NG12) ; This work was supported in part by grants from 863 Program (2006AA02A241) and the Outstanding Overseas Chinese Scholars Fund of the CAS for IMCAS, and from the CAS Program (KSCX1-YW-R-15, KSCX1-YW-R-24), 973 Program (2006CB504208, 2006CB504302), and Key Technological R&D Program of Yunnan (2004NG12)
文献类型	期刊论文
条目标识符	http://ir.kiz.ac.cn/handle/152453/6435
专题	科研部门_分子免疫药理学（郑永唐）科研部门_动物模型与人类重大疾病机理重点实验室
通讯作者	tienpo@sun.im.ac.cn; zhengyt@mail.kiz.ac.cn
作者单位	1.Center for Molecular Virology, Institute of Microbiology, Chinese Academy of Sciences, Beijing 100101, China 2.Laboratory of Molecular Immunopharmacology, Key Laboratory of Animal Models and Human Disease Mechanisms, Kunming Institute of Zoology, Chinese Academy of Sciences, Kunming 650223, China 3.Graduate School of the Chinese Academy of Sciences, Beijing 100039, China
推荐引用方式 GB/T 7714	Pang W,Wang RR,Yang LM,et al. Recombinant protein of heptad-repeat HR212, a stable fusion inhibitor with potent anti-HIV action in vitro[J]. Virology,2008,377(1):80-87.
APA	Pang W.,Wang RR.,Yang LM.,Liu CM.,Tien P*.,...&zhengyt@mail.kiz.ac.cn.(2008).Recombinant protein of heptad-repeat HR212, a stable fusion inhibitor with potent anti-HIV action in vitro.Virology,377(1),80-87.
MLA	Pang W,et al."Recombinant protein of heptad-repeat HR212, a stable fusion inhibitor with potent anti-HIV action in vitro".Virology 377.1(2008):80-87.

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