Small molecule HIV entry inhibitors targeting gp120 or gp41:research advances / 国际药学研究杂志

ABSTRACT

The envelope glycoprotein subunit gp120 and the transmembrane subunit gp41 of human immunodeficiency virus type 1(HIV-1)play important roles in the process of viral entry into target cells, and serve as key targets for developing HIV-1 entry inhibitors. Peptide HIV entry inhibitors, such as T20, are limited in clinical application due to the lack of oral properties. However, because of the possible oral administration and high bioavailability, small molecule compounds become more and more important in the research for HIV entry inhibitors. In this review, we summarize the recent advances in the development of small molecule HIV-1 entry inhibitors, including the NBD and BMS series of small-molecule inhibitors targeting gp120 as well as the NB-206 and ADS-J1 se- ries of small-molecule inhibitors targeting gp41. These small molecule inhibitors are promising compounds with research value, which lay a foundation for the design of more efficient and more reasonable small-molecule HIV-1 entry inhibitors.