Design, synthesis and evaluation of potential inhibitors of HIV gp120-CD4 interactions

被引：11
作者：
Boussard, C
Klimkait, T
Mahmood, N
Pritchard, M
Gilbert, IH
机构：
[1] Cardiff Univ, Welsh Sch Pharm, Cardiff CF10 3XF, S Glam, Wales
[2] Univ Basel, Inst Med Microbiol, CH-4003 Basel, Switzerland
[3] St Bartholomews & Royal London Sch Med & Dent, London E1 2AD, England
[4] Parke Davis Neurosci Res Ctr, Cambridge, England
来源：
BIOORGANIC & MEDICINAL CHEMISTRY LETTERS | 2004年 / 14卷 / 10期
基金：
英国工程与自然科学研究理事会;
关键词：
D O I：
10.1016/j.bmcl.2004.02.091
中图分类号：
R914 [药物化学];
学科分类号：
100701 ;
摘要：
This paper describes an approach to prevent HIV-cell fusion by disrupting the interaction between HIV protein gp120 and CD4 receptor. The CD4 residues Phe43 and Arg59 make important interactions with gp120. Small molecule analogues were made to mimic the crucial features of these residues. The analogues were assayed using a cellular 'FIGS' assay to measure inhibition of cell fusion and caused some inhibition. (C) 2004 Elsevier Ltd. All rights reserved.
引用
收藏
页码：2673 / 2676
页数：4
相关论文
共 25 条
[1]   URETHANE PROTECTED DERIVATIVES OF 1-GUANYLPYRAZOLE FOR THE MILD AND EFFICIENT PREPARATION OF GUANIDINES [J].
BERNATOWICZ, MS ;
WU, YL ;
MATSUEDA, GR .
TETRAHEDRON LETTERS, 1993, 34 (21) :3389-3392
[2]   Design, synthesis and evaluation of peptide libraries as potential anti-HIV compounds, via inhibition of gp120/cell membrane interactions, using the gp120/cd4/fab17 crystal structure [J].
Boussard, C ;
Doyle, VE ;
Mahmood, N ;
Klimkait, T ;
Pritchard, M ;
Gilbert, IH .
EUROPEAN JOURNAL OF MEDICINAL CHEMISTRY, 2002, 37 (11) :883-890
[3]  
Cooley LA, 2002, JOURNAL OF THE ASSOCIATION OF ASPHALT PAVING TECHNOLOGISTS, VOL 71, P1
[4]   THE CD4 (T4) ANTIGEN IS AN ESSENTIAL COMPONENT OF THE RECEPTOR FOR THE AIDS RETROVIRUS [J].
DALGLEISH, AG ;
BEVERLEY, PCL ;
CLAPHAM, PR ;
CRAWFORD, DH ;
GREAVES, MF ;
WEISS, RA .
NATURE, 1984, 312 (5996) :763-767
[5]  
Findlay J. A., 1967, CAN J CHEM, V45, P1014
[6]   Enfuvirtide, a new drug for HIV infection [J].
Fletcher, CV .
LANCET, 2003, 361 (9369) :1577-1578
[7]  
Greene T.W., 1991, PROTECTIVE GROUPS OR, V2nd
[8]  
Jiang SB, 2002, CURR PHARM DESIGN, V8, P563
[9]  
KARN J, 1995, HIV BIOCH MOL BIOL D, V2
[10]   Dissecting the mode of action of various HIV-inhibitor classes in a stable cellular system [J].
Klimkait, T ;
Stauffer, F ;
Lupo, E ;
Sonderegger-Rubli, C .
ARCHIVES OF VIROLOGY, 1998, 143 (11) :2109-2131
123