The Current Status and Challenges in the Development of Fusion Inhibitors as Therapeutics for HIV-1 Infection
| Autor: | Chang Liu, Jianjun Tan, Cun Xin Wang, Xiao Yi Zhang, Xue Ting Ma |
|---|---|
| Rok vydání: | 2013 |
| Předmět: |
Enfuvirtide
viruses Molecular Sequence Data HIV Infections Biology Gp41 Membrane Fusion Virus Viral envelope HIV Fusion Inhibitors Viral entry Drug Discovery medicine Humans Amino Acid Sequence Gene Pharmacology chemistry.chemical_classification virus diseases Lipid bilayer fusion Virology HIV Envelope Protein gp41 chemistry HIV-1 Glycoprotein medicine.drug |
| Zdroj: | Current Pharmaceutical Design. 19:1810-1817 |
| ISSN: | 1381-6128 |
| DOI: | 10.2174/1381612811319100005 |
| Popis: | 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. |
| Databáze: | OpenAIRE |
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