Use of multivalent glycodendrimers to inhibit the activity of human immunodeficiency virus
申请人:——
公开号:US20040180852A1
公开(公告)日:2004-09-16
The present invention relates to compositions and methods for inhibiting the interaction of a ligand and receptor. In particular, compositions are methods are provided for inhibition of interaction between a virus, especially HIV, and a receptor. Inhibition of such ligand/receptor interaction is advantageous in inhibiting infection of a cell with a virus. Further, an inhibitor of ligand/receptor interaction serves as a standard in assays of inhibition in vitro or in vivo. In a particular embodiment, a composition according to the invention includes a compound having the formula: [(X)—(Y)]
p
-Z where X is
1
and where Q1 and Q2 are each independently H, a bond to Y, or a bond to Z, where at least one of Q1 or Q2 is a bond to Y or a bond to Z; where R1, R4, R6 and R8 are each H; R2, R3, and R5 are each independently OH, OSO3D, or OPO3D, and R7 is CH20H, CH2OSO3D or CH2OPO3D; where D is H or a cation selected from the group consisting of: alkali metal cations, alkaline earth metal cations, ammonium cations, quaternary ammonium cations and amine cations; and where at least one of R2, R3, R5 and R7 is a sulfur or phosphate containing group; where Y is an optional linker, Z is a multivalent support, and p is an integer in the range of 1-2000 inclusive.
本发明涉及用于抑制配体和受体相互作用的组合物和方法。具体而言,提供了用于抑制病毒(特别是HIV)与受体之间相互作用的组合物和方法。抑制此类配体/受体相互作用有助于抑制细胞感染病毒。此外,配体/受体相互作用的抑制剂可作为体外或体内抑制测定的标准。在一个特定实施例中,根据本发明的组合物包括具有以下结构的化合物:[(X)—(Y)]
p
-Z,其中X为1,Q1和Q2分别独立地为H、与Y的键或与Z的键,其中Q1或Q2中至少有一个是与Y的键或与Z的键;R1、R4、R6和R8各自为H;R2、R3和R5各自独立地为OH、OSO3D或OPO3D,R7为CH20H、CH2OSO3D或CH2OPO3D;D为H或从以下群组中选择的阳离子:碱金属阳离子、碱土金属阳离子、铵阳离子、季铵阳离子和胺阳离子;其中R2、R3、R5和R7中至少有一个是含硫或磷酸酯基团;Y为可选的连接剂,Z为多价支持体,p为在1-2000范围内的整数。