HIV-1 variants with a single-point mutation in the gp41 pocket region exhibiting different susceptibility to HIV fusion inhibitors with pocket- or membrane-binding domain

Article ID	Journal	Published Year	Pages	File Type
8300017	Biochimica et Biophysica Acta (BBA) - Biomembranes	2012	8 Pages	PDF

Abstract

âº T20 contains membrane-binding domain (MBD) but lacks pocket-binding domain (PBD). âº We constructed pseudoviruses with mutations of A67 in gp41 NHR pocket region. âº These mutants are sensitive to T20 lacking PBD but resistant to C34 that contains PBD. âº Combining T20 & C34 lead to synergistic effect against T20- & C34-resistant mutants. âº These suggest that T20 and C34 inhibit HIV-1 fusion by binding to different targets.

Keywords

Hbd TCID50 NHR PBD gp41 Chr MBD ENV PFD IC50 50% tissue culture infective dose Native polyacrylamide gel electrophoresis Six-helix bundle mutation circular dichroism Membrane-binding concentration causing 50% inhibition Drug-resistance Fusion inhibitors HIV-1 Envelope protein