2l6t

Efficacy of an HIV-1 entry inhibitor targeting the GP41 fusion peptide

spinqualitylabelsall models 2l6t, 14 NMR models Show:Asymmetric Unit Biological Assembly Drag the structure with the mouse to rotate   Export Animated Image   Print3D Structural highlights 2l6t is a 1 chain structure. Full experimental information is available from OCA. For a guided tour on the structure components use FirstGlance. Related: 2jnr, 2l6s Resources: FirstGlance, OCA, RCSB, PDBsum Publication Abstract from PubMed To infect host cells, most enveloped viruses must insert a hydrophobic fusion peptide into the host cell membrane. Thus, fusion peptides may be valuable targets for developing drugs that block virus entry. We have shown previously that a natural 20-residue fragment of alpha(1)-antitrypsin, designated VIRus-Inhibitory Peptide (VIRIP), that binds to the gp41 fusion peptide of HIV-1 prevents the virus from entering target cells in vitro. Here, we examine the efficacy of 10-day monotherapy with the optimized VIR-576 derivative of VIRIP in treatment-naive, HIV-1-infected individuals with viral RNA loads of >/=10,000 copies per ml. We report that at the highest dose (5.0 grams per day), intravenous infusion of VIR-576 reduced the mean plasma viral load by 1.23 log(10) copies per ml without causing severe adverse effects. Our results are proof of concept that fusion peptide inhibitors suppress viral replication in human patients, and offer prospects for the development of a new class of drugs that prevent virus particles from anchoring to and infecting host cells. Short-term monotherapy in HIV-infected patients with a virus entry inhibitor against the gp41 fusion peptide.,Forssmann WG, The YH, Stoll M, Adermann K, Albrecht U, Barlos K, Busmann A, Canales-Mayordomo A, Gimenez-Gallego G, Hirsch J, Jimenez-Barbero J, Meyer-Olson D, Munch J, Perez-Castells J, Standker L, Kirchhoff F, Schmidt RE Sci Transl Med. 2010 Dec 22;2(63):63re3. PMID:21178138 From MEDLINE®/PubMed®, a database of the U.S. National Library of Medicine.

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