RANTES衍生物与HIV-1进入抑制剂

RANTES Derivates and HIV-1 Entry Inhibitor

HIV-1-1进入抑制剂的研究是近年来艾滋病药物研发领域的新热点,其中最受关注的是以CCR5为靶点的新药研发。CCR5是病毒进入细胞的主要辅助受体,在HIV-1进入宿主细胞过程中起着非常重要的作用。作为CCR5的天然配体,CC类的趋化因子RANTES、MIP-1α和MIP-1β都是极具潜力的HIV-1抑制剂,特别是有关对RANTES的定向设计的研究尤为引人关注,其目的是设计出一种既有很强的抗病毒能力而又不引发炎症反应的HIV-1拮抗剂。就RANTES衍生物应用于抑制HIV进入细胞方面的研究进行了综述。

HIV-1 entry inhibitor is a new hot spot in the area of AIDS drug development. The identification of CCR5 as the main HIV co-receptor have triggered a wealth of research about CCR5-targeting inhibitors. Natural ligands of CCR5, RANTES, MIP-Iot, and MIP-1β are potent HIV-1 inhibitors. Lots of efforts have focused on RANTES engineering aiming at enhancing the antivirus ability of the native molecule, while reducing its side effect. Here an overview of RANTES derivates developed as HIV-1 entry inhibitors is presented.