HIV-1逆转录酶抑制剂的新进展(2021—2023年)

New Progress in HIV-1 Reverse Transcriptase Inhibitors(2021—2023)

逆转录酶可将病毒的单链RNA逆转录成双链DNA,在人类免疫缺陷病毒1型(HIV-1)的复制周期中发挥着不可替代的作用。逆转录酶抑制剂作为高效抗逆转录病毒疗法的重要组分,在治疗艾滋病方面取得了巨大的成功,大大降低了HIV-1患者的发病率和死亡率。然而,随着逆转录酶抑制剂在临床中的长期应用,许多问题逐渐显露,如耐药性和不良反应等。因此,开发出新型高效低毒和抗耐药性的逆转录酶抑制剂具有重要意义。通过对近3年靶向HIV-1逆转录酶的抗艾滋病药物及相关候选药物的最新研究进展进行综述,以期为新型逆转录酶抑制剂的发现提供参考。

Reverse transcriptase(RT),which reverse-transcribes viral single-stranded RNA into double-stranded DNA,plays an irreplaceable role in the replication cycle of human immunodeficiency virus type 1(HIV-1).Reverse transcriptase inhibitors(RTIs),a key component of highly active antiretroviral therapy(HAART),have achieved great success in the treatment of AIDS,drastically reducing the morbidity and mortality of HIV-infected patients.However,with the long-term application of RTIs in clinic,many problems,such as drug resistance and adverse reaction,have gradually emerged.Therefore,it is of great significance to develop novel HIV-1 RTIs with high efficiency,low toxicity and anti-drug resistance.In this review,the latest research progress of anti-AIDS drugs and related drug candidates targeting HIV-1 RT in the past three years is summarized,aiming to provide some reference for further research and development of novel RTIs.