Fantini J, Yahi N, Mabrouk K, Van Rietschoten J, Rochat H, Sabatier J M
CNRS URA 1455, Laboratoire de Biochimie, Ingénierie des Protéines, Faculté de Médecine Secteur Nord, Marseille, France.
C R Acad Sci III. 1993 Nov;316(11):1381-7.
The V3 loop is an hypervariable region of the HIV-1 surface envelope glycoprotein gp120 that is able to generate neutralizing antibodies. These antibodies are generally type-specific. They inhibit the interaction between the V3 loop and the membrane molecules involved in virus-cell and cell-cell fusion. Synthetic peptides based on the V3 loop sequence have been tentatively used to block the fusion process, but the results were unsuccessful. In this report, we confirm that monomeric V3 peptides are devoid of any anti-HIV activity. However, we found that, when assembled in a synthetic polymeric construction (SPC), these peptides have been able to inhibit the infection of human CD4+ lymphocytes and macrophages as well as CD4- epithelial intestinal cells by distantly related isolates of HIV-1 and HIV-2. V3 SPCs, based on the consensus HIV-1 sequence, may therefore represent a new class of therapeutically useful anti-HIV agents able to neutralize a wide range of viral isolates in both CD4+ and CD4- susceptible cells.
V3环是HIV-1表面包膜糖蛋白gp120的一个高变区，能够产生中和抗体。这些抗体通常具有型特异性。它们抑制V3环与参与病毒-细胞和细胞-细胞融合的膜分子之间的相互作用。基于V3环序列的合成肽曾被尝试用于阻断融合过程，但结果并不成功。在本报告中，我们证实单体V3肽没有任何抗HIV活性。然而，我们发现，当组装成合成聚合物结构（SPC）时，这些肽能够抑制HIV-1和HIV-2的远亲分离株对人CD4+淋巴细胞、巨噬细胞以及CD4-肠上皮细胞 的感染。因此，基于HIV-1共有序列的V3 SPC可能代表一类新型的具有治疗作用的抗HIV药物，能够在CD4+和CD4-易感细胞中中和多种病毒分离株。
