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Despite advances in the development of potent antiretroviral regimens that block HIV transcription and assembly, problems of drug resistance, latent viral reservoirs and drug-induced toxic effects that compromise effective viral control all point to the need for new classes of anti-HIV drugs with different modes of action. One promising approach involves blocking HIV entry into cells.
The process of HIV entry begins with binding of the viral envelope glycoprotein to both the CD4 receptor and one of only two chemokine receptors, and ends with fusion of viral and cell membranes. Viral entry provides novel therapeutic targets against HIV. To date, at least 3 sub-classes of HIV viral entry/fusion inhibitors have emerged:
CD4 binding or attachment — targets initial recognition and binding of the viral glycoprotein gp120 to the cell-surface CD4 antigen.
Chemokine co-receptor binding — targets binding of virus to the CCR5 or CXCR4 co-receptor.
Fusion inhibition — targets the viral...