Lacoux X, Barragan V, Dewynter G, Leydet A, Roque J P, Montero J L
Laboratoires de Chimie Biomoléculaire, Université de Montpellier-II, France.
Farmaco. 1996 Dec;51(12):767-73.
In order to inhibit the gp 120-CD4 glycoprotein interaction, a key step of the HIV-infection, we have synthesized a series of N-acylated peptides containing sequences identified in both the viral and lymphocytic proteins, (SDFR, SDAR, RFDSAARFDS, DRADSRRS, PSKLNDRADSRRSLWD, ASTTTNYT). An hydrophobic moiety (capryloyl, palmitoyl acrylamidoundecanoyl) was introduced in the last step of interactive synthesis, in homogeneous or solid phase. The acrylogyl-containing compounds were then telomerized under UV irradiation (DPn observed: 2 to 6). The biological evaluation shown an antiviral effect in vitro for telomerized peptides containing amino diacids such as Glu and Asp.
为了抑制HIV感染的关键步骤——gp120-CD4糖蛋白相互作用，我们合成了一系列N-酰化肽，其包含在病毒蛋白和淋巴细胞蛋白中均已鉴定出的序列（SDFR、SDAR、RFDSAARFDS、DRADSRRS、PSKLNDRADSRRSLWD、ASTTTNYT）。在交互式合成的最后一步，在均相或固相中引入了一个疏水部分（辛酰基、棕榈酰基、丙烯酰胺基十一烷酰基）。然后，含丙烯酰基的化合物在紫外线照射下进行端粒化反应（观察到的聚合度：2至6）。生物学评估表明，含有诸如Glu和Asp等氨基酸二酸的端粒化肽在体外具有抗病毒作用。
