Design and evaluation of antiretroviral peptides corresponding to the C-terminal heptad repeat region (C-HR) of human immunodeficiency virus type 1 envelope glycoprotein gp41

被引：3

作者：

Soonthornsata, Bongkot ^{[1
]}

Tian, Yu-Shi ^{[2
]}

Utachee, Piraporn ^{[1
]}

Sapsutthipas, Sompong ^{[1
]}

Isarangkura-na-ayuthaya, Panasda ^{[3
]}

Auwanit, Wattana ^{[3
]}

Takagi, Tatsuya ^{[1
,2
]}

Ikuta, Kazuyoshi ^{[1
,4
]}

Sawanpanyalert, Pathom ^{[3
]}

Kawashita, Norihito ^{[1
,2
]}

Kameoka, Masanori ^{[1
,4
]}

机构：

[1] Thailand Japan Res Collaborat Ctr Emerging & Reem, Nonthaburi, Thailand

[2] Osaka Univ, Grad Sch Pharmaceut Sci, Osaka, Japan

[3] Minist Publ Hlth, Dept Med Sci, Natl Inst Hlth, Nonthaburi 11000, Thailand

[4] Osaka Univ, Dept Virol, Microbial Dis Res Inst, Osaka, Japan

来源：

VIROLOGY | 2010年 / 405卷 / 01期

关键词：

HIV-1; Envelope glycoprotein gp41; alpha-helical heptad repeat; C34 fusion inhibitor; CRF01_AE; Subtypes; HIV-1 FUSION INHIBITOR; RESISTANT HIV-1; ENV CLONES; ENFUVIRTIDE; INFECTIONS; CORE; T-20; EMERGENCE; ENTRY;

D O I：

10.1016/j.virol.2010.06.012

中图分类号：

Q93 [微生物学];

学科分类号：

071005 ; 100705 ;

摘要：

Two alpha-helical heptad repeats. N-HR and C-HR, located in the human immunodeficiency virus type 1 (HIV-1) envelope glycoprotein gp41, play an important role in membrane fusion by forming a 6-helix bundle. C34, a peptide mimicking C-HR, inhibits the formation of the 6-helix bundle, thus, it has potential as a novel antiretroviral compound In order to improve the inhibitory effect of C34 on HIV-1 replication, we designed new C34-derived peptides based on computational analysis of the stable conformation of the 6-helix bundle Newly designed peptides showed a stronger inhibitory effect on the replication of recombinant viruses containing CRF01_AE, subtype B or subtype C Env than C34 or a fusion inhibitor, T-20 In addition, these peptides inhibited the replication of a T-20-resistant virus We propose that these peptides could be applied to develop novel antiretroviral compounds to inhibit the replication of various subtypes of HIV-I as well as of T-20-resistant variants (C) 2010 Elsevier Inc All rights reserved

引用

页码：157 / 164

页数：8

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