Stapled peptide-based membrane fusion inhibitors of hepatitis C virus

被引：61

作者：

Cui, Hong-Kui ^{[1
]}

Qing, Jie ^{[1
]}

Guo, Ye ^{[1
]}

Wang, Yu-Jia ^{[1
]}

Cui, Li-Jia ^{[2
,3
]}

He, Tian-Hua ^{[2
,3
]}

Zhang, Linqi ^{[2
,3
]}

Liu, Lei ^{[1
]}

机构：

[1] Tsinghua Univ, Dept Chem, Tsinghua Peking Ctr Life Sci,Minist Educ, Key Lab Bioorgan Phosphorus Chem & Chem Biol, Beijing 100084, Peoples R China

[2] Tsinghua Univ, Sch Med, Comprehens AIDS Res Ctr, Beijing 100084, Peoples R China

[3] Tsinghua Univ, Sch Med, Res Ctr Publ Hlth, Beijing 100084, Peoples R China

来源：

BIOORGANIC & MEDICINAL CHEMISTRY | 2013年 / 21卷 / 12期

基金：

中国国家自然科学基金;

关键词：

Hepatitis C virus; Stapled peptide; Protein-protein interaction; CELL-CULTURE SYSTEMS; B TYPE-I; OLEFIN METATHESIS; ALPHA-HELICES; BH3; HELIX; CD81; ENTRY; INFECTION; PROTEINS; RECEPTOR;

D O I：

10.1016/j.bmc.2013.02.011

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：

The strategy of peptide stapling was used to develop new molecules to inhibit the hepatitis C virus infection via disrupting the binding of HCV envelope glycoprotein E2 with human cell surface protein CD81. The peptide sequence was designed based on the large extra-cellular loop of CD81 with known importance in the HCV E2 binding interaction. Our results showed that the stapled peptides exhibited significantly higher alpha-helicity and proteolytic stability as compared to their linear peptide counterpart. The optimal compound was found to have an EC50 value of ca. 17-39 mu M against different HCV subtypes and represented a new HCV membrane fusion inhibitor. (C) 2013 Elsevier Ltd. All rights reserved.

引用

下载

页码：3547 / 3554

页数：8

共 50 条

[1] Peptide-based inhibitors of the hepatitis C virus serine protease
Llinàs-Brunet, M
Bailey, M
Fazal, G
Goulet, S
Halmos, T
Laplante, S
Maurice, R
Poirier, M
Poupart, MA
Thibeault, D
Wernic, D
Lamarre, D
BIOORGANIC & MEDICINAL CHEMISTRY LETTERS, 1998, 8 (13) : 1713 - 1718
[2] Small peptide-based inhibitors of the hepatitis C virus serine protease.
Narjes, F
Colarusso, S
Gerlach, B
Koehler, K
Koch, U
Steinkühler, C
Bazzo, R
Sollazzo, M
Altamura, S
De Francesco, R
Matassa, VG
ABSTRACTS OF PAPERS OF THE AMERICAN CHEMICAL SOCIETY, 2000, 220 : U539 - U540
[3] Highly potent and selective peptide-based inhibitors of the hepatitis C virus serine protease:: Towards smaller inhibitors
Llinàs-Brunet, M
Bailey, M
Fazal, G
Ghiro, E
Gorys, V
Goulet, S
Halmos, T
Maurice, R
Poirier, M
Poupart, MA
Rancourt, J
Thibeault, D
Wernic, D
Lamarre, D
BIOORGANIC & MEDICINAL CHEMISTRY LETTERS, 2000, 10 (20) : 2267 - 2270
[4] Perspectives: towards a peptide-based vaccine against hepatitis C virus
Hunziker, IP
Zurbriggen, R
Glueck, R
Engler, OB
Reichen, J
Dai, WJ
Pichler, WJ
Cerny, A
MOLECULAR IMMUNOLOGY, 2001, 38 (06) : 475 - 484
[5] Peptide-based inhibition of HCMV through blocking virus: Cell membrane fusion
Melnik, Lilia I.
Garry, Robert F.
Morris, Cindy A.
PLACENTA, 2008, 29 (08) : A25 - A25
[6] Optimisation of peptide-based inhibitors of full-length hepatitis C virus NS3 protease
Poliakov, A
Johansson, A
Åkerblom, E
Lindeberg, G
Hallberg, A
Danielson, UH
ANTIVIRAL RESEARCH, 2004, 62 (02) : A51 - A51
[7] Transmembrane peptide-based inhibitors of membrane protein folding and function
Melnyk, RA
Partridge, AW
Yang, D
Bowie, JU
Deber, CM
BIOPOLYMERS, 2003, 71 (03) : 279 - 279
[8] Peptide-based inhibitors of the hepatitis C virus NS3 protease:: Structure-activity relationship at the C-terminal position
Rancourt, J
Cameron, DR
Gorys, V
Lamarre, D
Poirier, M
Thibeault, D
Llinàs-Brunet, M
JOURNAL OF MEDICINAL CHEMISTRY, 2004, 47 (10) : 2511 - 2522
[9] Cholesterol alters the inhibitory efficiency of peptide-based membrane fusion inhibitor
Pattnaik, Gourab Prasad
Chakraborty, Hirak
BIOCHIMICA ET BIOPHYSICA ACTA-BIOMEMBRANES, 2019, 1861 (12):
[10] Flunarizine arrests hepatitis C virus membrane fusion
Prigozhin, Daniil M.
Modis, Yorgo
HEPATOLOGY, 2016, 63 (01) : 14 - 16

← 1 2 3 4 5 →