Identification of a β3-peptide HIV fusion inhibitor with improved potency in live cells

被引：30
|
作者：
Bautista, Arjel D. [1 ]
Stephens, Olen M. [1 ]
Wang, Ligong [3 ]
Domaoal, Robert A. [3 ]
Anderson, Karen S. [3 ]
Schepartz, Alanna [1 ,2 ]
机构：
[1] Yale Univ, Dept Chem, New Haven, CT 06520 USA
[2] Yale Univ, Dept Mol Cellular & Dev Biol, New Haven, CT 06520 USA
[3] Yale Univ, Sch Med, Dept Pharmacol, New Haven, CT 06510 USA
来源：
BIOORGANIC & MEDICINAL CHEMISTRY LETTERS | 2009年 / 19卷 / 14期
关键词：
Foldamer; Peptidomimetic; Anti-viral; Drug design; IMMUNODEFICIENCY-VIRUS TYPE-1; D-PEPTIDE INHIBITORS; BETA-PEPTIDES; IN-VITRO; HTLV-III; ELECTROSTATIC INTERACTIONS; ATOMIC-STRUCTURE; CORE STRUCTURE; COILED-COIL; GP41;
D O I：
10.1016/j.bmcl.2009.05.032
中图分类号：
R914 [药物化学];
学科分类号：
100701 ;
摘要：
We recently reported a beta(3)-decapeptide, beta WWI-1, that binds a validated gp41 model in vitro and inhibits gp41-mediated fusion in cell culture. Here we report six analogs of beta WWI-1 containing a variety of non-natural side chains in place of the central tryptophan of the WWI-epitope. These analogs were compared on the basis of both gp41 affinity in vitro and fusion inibition in live, HIV-infected cells. One new beta(3)-peptide, beta WXI-a, offers a significantly improved CC50/EC50 ratio in the live cell assay. (C) 2009 Elsevier Ltd. All rights reserved.
引用
收藏
页码：3736 / 3738
页数：3
相关论文
共 50 条
  • [41] Molecular Dynamics Simulation of HIV Fusion Inhibitor T-1249: Insights on Peptide-Lipid Interaction
    Martins do Canto, A. M. T.
    Palace Carvalho, A. J.
    Prates Ramalho, J. P.
    Loura, Luis M. S.
    COMPUTATIONAL AND MATHEMATICAL METHODS IN MEDICINE, 2012, 2012
  • [42] The synthesis of a 60mer peptide for investigating the mechanism of action of the HIV fusion inhibitor T20
    Chandramouli, Nagarajan
    Powell, Susan
    Jing, Weiguo
    Deng, Haiteng
    Jiang, Shibo
    JOURNAL OF PEPTIDE SCIENCE, 2008, 14 (08) : 91 - 91
  • [43] Discovery and optimization of a natural HIV-1 entry inhibitor targeting the gp41 fusion peptide
    Muench, Jan
    Staendker, Ludger
    Adermann, Knut
    Schuz, Axel
    Schindler, Michael
    Chinnadurai, Raghavan
    Poehlmann, Stefan
    Chaipan, Chawaree
    Biet, Thorsten
    Peters, Thomas
    Meyer, Bernd
    Wilhelm, Dennis
    Lu, Hong
    Jing, Weiguo
    Jiang, Shibo
    Forssmann, Wolf-Georg
    Kirchhoff, Frank
    CELL, 2007, 129 (02) : 263 - 275
  • [44] Short-peptide fusion inhibitors with high potency against wild-type and enfuvirtide-resistant HIV-1
    Chong, Huihui
    Yao, Xue
    Qiu, Zonglin
    Sun, Jianping
    Zhang, Meng
    Waltersperger, Sandro
    Wang, Meitian
    Liu, Shan-Lu
    Cui, Sheng
    He, Yuxian
    FASEB JOURNAL, 2013, 27 (03): : 1203 - 1213
  • [45] Quantitative FRET-FLIM-BlaM to Assess the Extent of HIV-1 Fusion in Live Cells
    Carlon-Andres, Irene
    Padilla-Parra, Sergi
    VIRUSES-BASEL, 2020, 12 (02):
  • [46] Identification and optimization of VIRIP -: A natural occurring peptide blocking HIV-1 entry by interfering with the Gp41 fusion peptide
    Muench, J
    Ständker, L
    Adermann, K
    Schulz, A
    Schindler, M
    Chinnadurai, R
    Forssmann, WG
    Kirchoff, F
    ANTIVIRAL RESEARCH, 2006, 70 (01) : A28 - A28
  • [47] Evaluation of the fusion inhibitor P3 peptide as a potential microbicide to prevent HIV transmission in women (vol 13, e0195744, 2018)
    Bartolo, Ines
    Diniz, Ana Rita
    Borrego, Pedro
    Ferreira, Joao Pedro
    Bronze, Maria Rosario
    Barroso, Helena
    Pinto, Rui
    Cardoso, Carlos
    Pinto, Joao F.
    Diaz, Rafael Cena
    Broncano, Pilar Garcia
    Munoz-Fernandez, Maria Angel
    Taveira, Nuno
    PLOS ONE, 2018, 13 (05):
  • [48] Exceptional potency and structural basis of a T1249-derived lipopeptide fusion inhibitor against HIV-1, HIV-2, and simian immunodeficiency virus
    Zhu, Yuanmei
    Zhang, Xiujuan
    Ding, Xiaohui
    Chong, Huihui
    Cui, Sheng
    He, Jinsheng
    Wang, Xinquan
    He, Yuxian
    JOURNAL OF BIOLOGICAL CHEMISTRY, 2018, 293 (14) : 5323 - 5334
  • [49] Identification of a Human Protein-Derived HIV-1 Fusion Inhibitor Targeting the gp41 Fusion Core Structure
    Chao, Lijun
    Lu, Lu
    Yang, Hengwen
    Zhu, Yun
    Li, Yuan
    Wang, Qian
    Yu, Xiaowen
    Jiang, Shibo
    Chen, Ying-Hua
    PLOS ONE, 2013, 8 (05):
  • [50] A Protein-Based, Long-Acting HIV-1 Fusion Inhibitor with an Improved Pharmacokinetic Profile
    Xu, Wei
    Cong, Zhe
    Duan, Qianyu
    Wang, Qian
    Su, Shan
    Wang, Rui
    Lu, Lu
    Xue, Jing
    Jiang, Shibo
    PHARMACEUTICALS, 2022, 15 (04)
12345