title: The current status and challenges in the development of fusion inhibitors as therapeutics for HIV-1 infection.
abstract: 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.
authors.affiliation: College of Life Science and Bio-engineering, Beijing University of Technology, Beijing 100124, China. tanjianjun@bjut.edu.cn
authors.forename: Jian Jun
authors.initials: JJ
authors.lastname: Tan
authors.forename: Xue Ting
authors.initials: XT
authors.lastname: Ma
authors.forename: Chang
authors.initials: C
authors.lastname: Liu
authors.forename: Xiao Yi
authors.initials: XY
authors.lastname: Zhang
authors.forename: Cun Xin
authors.initials: CX
authors.lastname: Wang
mesh_terms: D000595:Amino Acid Sequence; D015700:HIV Envelope Protein gp41 / Q000737:chemistry; D023581:HIV Fusion Inhibitors / Q000737:chemistry / Q000494:pharmacology / Q000627:therapeutic use*; D015658:HIV Infections / Q000188:drug therapy*; D015497:HIV-1 / Q000187:drug effects* / Q000502:physiology; D006801:Humans; D008561:Membrane Fusion / Q000187:drug effects*; D008969:Molecular Sequence Data
chemical_list: D015700:HIV Envelope Protein gp41; D023581:HIV Fusion Inhibitors