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HIV-1融合抑制剂是继逆转录酶和蛋白酶抑制剂后的新一类抗HIV感染药物,通过阻断病毒与靶细胞膜的融合从而抑制病毒进入靶细胞,在感染的初始环节切断HIV-1的传播,其中多肽类融合抑制剂T-20已于2003年上市。HIV-1融合抑制剂以HIV-1跨膜糖蛋白gp41为作用靶标,它们是一些天然或合成的多肽以及小分子化合物,通过与gp41功能区结合从而抑制其促融合功能的发挥。近年来,随着对膜融合过程分子机制以及gp41功能研究的不断深入,新的以gp41不同功能区为靶点的融合抑制剂分子不断被发现,成为倍受关注的研究热点之一。本文着重对近年来HIV-1融合抑制剂的研究现状及发展趋势进行综述。
HIV-1 fusion inhibitor is a new class of anti-HIV drug following reverse transcriptase and protease inhibitors, which blocks the entry of virus into target cells by blocking the fusion of the virus with the target cell membrane, cutting off HIV-1 at the initial stage of infection Of which the polypeptide fusion inhibitor T-20 was marketed in 2003. HIV-1 fusion inhibitors target HIV-1 transmembrane glycoprotein gp41, which are natural or synthetic peptides and small molecule compounds that inhibit their fusogenic function by binding to the gp41 domain. In recent years, with the further research on the molecular mechanism of membrane fusion and the function of gp41, new fusion inhibitor molecules targeting different functional domains of gp41 are continuously discovered and become one of the hot spots of great concern. This article focuses on the research status and development trend of HIV-1 fusion inhibitors in recent years.