Skip to main content
padlock icon - secure page this page is secure

Inhibition of HIV-1 by Fusion Inhibitors

Buy Article:

$68.00 + tax (Refund Policy)

The envelope glycoprotein complex (Env) is responsible for entry of the human immunodeficiency virus type 1 (HIV-1) into cells by mediating attachment to target cells and subsequent membrane fusion. Env consists of three gp120 subunits that mediate receptor and co-receptor attachment and three gp41 subunits responsible for membrane fusion. Several steps of the entry process can serve as drug targets. Receptor antagonists prevent attachment of gp120 to the receptor or co-receptor and conformational changes within gp41 required for membrane fusion can be inhibited by fusion inhibitors. Enfuvirtide (T20, Fuzeon) is a peptide based on the gp41 sequence and is the only approved fusion inhibitor. It prevents membrane fusion by competitively binding to gp41 and blocking the formation of the post-fusion structure. New generations of T20-like peptides have been developed with improved potency and stability. Besides T20 and derivatives, other fusion inhibitors have been developed that target different domains of gp41. Here we discuss the development of fusion inhibitors, their mode of action and their potential for incorporation in future drug regimens.





No References
No Citations
No Supplementary Data
No Article Media
No Metrics

Keywords: BMS-378806; Cyclic depsipeptides; DNA strand elongation; Enfuvirtide; Fusion Inhibitors; Fuzeon; Gag-Pol precursor; HIV; HIV-1; HXB2 isolate; Highly Active Antiretroviral Therapy (HAART); Maraviroc; N126K; PRO542; S138A; Saquinavir; Siliquaria spongia mirabilis; T20; TORO phase III study; VIRIP; abacavir; acquired immunodeficiency syndrome; antiviral peptide; coronaviridae; didanosine; enfuvirtide; envelope glycoprotein complex; fusion inhibitors; gp120; gp41; guanine; human immunodeficiency virus type 1; immunoglobulin; indinavir; integrase; non-nucleoside RT inhibitors; nucleoside analogue; resistance; reverse transcriptase (RT); ritonavir; stavudine; thymidine; vicriviroc; viral Gag; virus entry; zidovudine

Document Type: Research Article

Publication date: November 1, 2010

More about this publication?
  • Current Pharmaceutical Design publishes timely in-depth reviews covering all aspects of current research in rational drug design. Each issue is devoted to a single major therapeutic area. A Guest Editor who is an acknowledged authority in a therapeutic field has solicits for each issue comprehensive and timely reviews from leading researchers in the pharmaceutical industry and academia.

    Each thematic issue of Current Pharmaceutical Design covers all subject areas of major importance to modern drug design, including: medicinal chemistry, pharmacology, drug targets and disease mechanism.
  • Editorial Board
  • Information for Authors
  • Subscribe to this Title
  • Ingenta Connect is not responsible for the content or availability of external websites
  • Access Key
  • Free content
  • Partial Free content
  • New content
  • Open access content
  • Partial Open access content
  • Subscribed content
  • Partial Subscribed content
  • Free trial content
Cookie Policy
X
Cookie Policy
Ingenta Connect website makes use of cookies so as to keep track of data that you have filled in. I am Happy with this Find out more