Generic placeholder image

Current Pharmaceutical Design


ISSN (Print): 1381-6128
ISSN (Online): 1873-4286

The Current Status and Challenges in the Development of Fusion Inhibitors as Therapeutics for HIV-1 Infection

Author(s): Jian Jun Tan, Xue Ting Ma, Chang Liu, Xiao Yi Zhang and Cun Xin Wang

Volume 19, Issue 10, 2013

Page: [1810 - 1817] Pages: 8

DOI: 10.2174/1381612811319100005

Price: $65


HIV-1 membrane fusion as a part of the process of viral entry in the target cells is facilitated by gp41 and gp120, which are encoded by Env gene of HIV-1. Based on the structure and the mechanism researches, new treatment options targeting HIV-1 entry process have been proposed. Enfuvirtide, which mimics amino acid sequences of viral envelope glycoprotein gp41, is the first HIV-1 fusion inhibitor approved by FDA. Although it fulfills vital functions by binding to gp41 and abolishing the membrane fusion reaction when used in combination, it could induce drug resistant virus variants. Currently, a number of design and modification schemes have been presented, a large number of prospective fusion peptides have emerged. For these fusion inhibitors, multiple mutations in gp41 have been associated with the loss of susceptibility to agents. This review reported the current developments and innovative designs of HIV-1 membrane fusion inhibitors.

Keywords: HIV-1, gp41, gp120, fusion inhibitor

Rights & Permissions Print Export Cite as
© 2023 Bentham Science Publishers | Privacy Policy