靶向HIV-1跨膜蛋白gp41的多肽类融合抑制剂的研究进展

Research Progress in Polypeptide Fusion Inhibitors Targeting HIV-1 Transmembrane Protein gp41

跨膜蛋白gp41是治疗获得性免疫缺陷综合征的重要靶点。恩夫韦肽是首个被FDA批准的以gp41为靶点的多肽类融合抑制剂。然后,恩夫韦肽较短的半衰期、较低的耐药遗传屏障和较低的效力限制了它的临床应用。近年来,以gp41为作用靶点开发出来的多肽类融合抑制剂表现出了较好的效力和稳定性。为此,笔者主要对靶向跨膜蛋白gp41的多肽类融合抑制剂的研究状况进行了综述。

Transmembrane protein gp41 is an important target for the treatment of acquired immunodeficiency syndromes.Enfuvirtide is the first polypeptide fusion inhibitor targeting gp41 approved by FDA.However,with relatively short half-life,relatively low genetic barrier to drug resistance and low efficacy,the clinical use of enfuvirtide has been limited.In recent years,polypeptide fusion inhibitors developed to target gp41 have demonstrated promising efficacy and stability.In this regard,this article mainly reviews the research status of polypeptide fusion inhibitors targeting transmembrane protein gp41.