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
  • [1] Toward a live microbial microbicide for HIV: Commensal bacteria secreting an HIV fusion inhibitor peptide
    Rao, S
    Hu, S
    McHugh, L
    Lueders, K
    Henry, K
    Zhao, Q
    Fekete, RA
    Kar, S
    Adhya, S
    Hamer, DH
    PROCEEDINGS OF THE NATIONAL ACADEMY OF SCIENCES OF THE UNITED STATES OF AMERICA, 2005, 102 (34) : 11993 - 11998
  • [2] Sifuvirtide, a potent HIV fusion inhibitor peptide
    Wang, Rui-Rui
    Yang, Liu-Meng
    Wang, Yun-Hua
    Pang, Wei
    Tam, Siu-Cheung
    Tien, Po
    Zheng, Yong-Tang
    BIOCHEMICAL AND BIOPHYSICAL RESEARCH COMMUNICATIONS, 2009, 382 (03) : 540 - 544
  • [3] A novel peptide shows excellent anti-HIV-1 potency as a gp41 fusion inhibitor
    Liu, Wei
    An, Xiaohong
    Wang, Jiao
    Zhang, Xiaoguang
    Tan, Jianjun
    Zhou, Zhixiang
    Zeng, Yi
    BIOORGANIC & MEDICINAL CHEMISTRY LETTERS, 2018, 28 (05) : 910 - 914
  • [4] Addition of a cholesterol group to an HIV-1 peptide fusion inhibitor dramatically increases its antiviral potency
    Ingallinella, Paolo
    Bianchi, Elisabetta
    Ladwa, Neal A.
    Wang, Ying-Jie
    Hrin, Renee
    Veneziano, Maria
    Bonelli, Fabio
    Ketas, Thomas J.
    Moore, John P.
    Miller, Michael D.
    Pessi, Antonello
    PROCEEDINGS OF THE NATIONAL ACADEMY OF SCIENCES OF THE UNITED STATES OF AMERICA, 2009, 106 (14) : 5801 - 5806
  • [5] DRAMATIC INCREASE OF ANTIVIRAL POTENCY OF AN HIV PEPTIDE FUSION INHIBITOR BY TARGETING TO LIPID RAFTS VIA ADDITION OF A CHOLESTEROL GROUP
    Pessi, A.
    Ingallinella, P.
    Bianchi, E.
    Wang, Y. -J.
    Hrin, R.
    Veneziano, M.
    Bonelli, F.
    Ketas, T.
    Moore, J.
    Miller, M.
    BIOPOLYMERS, 2009, 92 (04) : 302 - 302
  • [6] Adding an Artificial TailAnchor to a Peptide-Based HIV-1 Fusion Inhibitor for Improvement of Its Potency and Resistance Profile
    Su, Shan
    Ma, Zhenxuan
    Hua, Chen
    Li, Weihua
    Lu, Lu
    Jiang, Shibo
    MOLECULES, 2017, 22 (11):
  • [7] Modular assembly of dimeric HIV fusion inhibitor peptides with enhanced antiviral potency
    Xiao, Junpeng
    Tolbert, Thomas J.
    BIOORGANIC & MEDICINAL CHEMISTRY LETTERS, 2013, 23 (22) : 6046 - 6051
  • [8] Improved Pharmacological and Structural Properties of HIV Fusion Inhibitor AP3 over Enfuvirtide: Highlighting Advantages of Artificial Peptide Strategy
    Zhu, Xiaojie
    Zhu, Yun
    Ye, Sheng
    Wang, Qian
    Xu, Wei
    Su, Shan
    Sun, Zhiwu
    Yu, Fei
    Liu, Qi
    Wang, Chao
    Zhang, Tianhong
    Zhang, Zhenqing
    Zhang, Xiaoyan
    Xu, Jianqing
    Du, Lanying
    Liu, Keliang
    Lu, Lu
    Zhang, Rongguang
    Jiang, Shibo
    SCIENTIFIC REPORTS, 2015, 5
  • [9] Improved Pharmacological and Structural Properties of HIV Fusion Inhibitor AP3 over Enfuvirtide: Highlighting Advantages of Artificial Peptide Strategy
    Xiaojie Zhu
    Yun Zhu
    Sheng Ye
    Qian Wang
    Wei Xu
    Shan Su
    Zhiwu Sun
    Fei Yu
    Qi Liu
    Chao Wang
    Tianhong Zhang
    Zhenqing Zhang
    Xiaoyan Zhang
    Jianqing Xu
    Lanying Du
    Keliang Liu
    Lu Lu
    Rongguang Zhang
    Shibo Jiang
    Scientific Reports, 5
  • [10] An artificial peptide-based HIV-1 fusion inhibitor containing M-T hook structure exhibiting improved antiviral potency and drug resistance profile
    Zhu, Xiaojie
    Yu, Fei
    Liu, Keliang
    Lu, Lu
    Jiang, Shibo
    FUTURE VIROLOGY, 2015, 10 (08) : 961 - 969
12345