AMD3100, a small molecule inhibitor of HIV-1 entry via the CXCR4 co-receptor
GA Donzella, D Schols, SW Lin, JA Esté… - Nature medicine, 1998 - nature.com
GA Donzella, D Schols, SW Lin, JA Esté, KA Nagashima, PJ Maddon, GP Allaway…
Nature medicine, 1998•nature.comThe bicyclam AMD3100 (formula weight 830) blocks HIV-1 entry and membrane fusion via
the CXCR4 co-receptor, but not via CCR5. AMD3100 prevents monoclonal antibody 12G5
from binding to CXCR4, but has no effect on binding of monoclonal antibody 2D7 to CCR5. It
also inhibits binding of the CXC-chemokine, SDF-1α, to CXCR4 and subsequent signal
transduction, but does not itself cause signaling and has no effect on RANTES signaling via
CCR5. Thus, AMD3100 prevents CXCR4 functioning as both a HIV-1 co-receptor and a …
the CXCR4 co-receptor, but not via CCR5. AMD3100 prevents monoclonal antibody 12G5
from binding to CXCR4, but has no effect on binding of monoclonal antibody 2D7 to CCR5. It
also inhibits binding of the CXC-chemokine, SDF-1α, to CXCR4 and subsequent signal
transduction, but does not itself cause signaling and has no effect on RANTES signaling via
CCR5. Thus, AMD3100 prevents CXCR4 functioning as both a HIV-1 co-receptor and a …
Abstract
The bicyclam AMD3100 (formula weight 830) blocks HIV-1 entry and membrane fusion via the CXCR4 co-receptor, but not via CCR5. AMD3100 prevents monoclonal antibody 12G5 from binding to CXCR4, but has no effect on binding of monoclonal antibody 2D7 to CCR5. It also inhibits binding of the CXC-chemokine, SDF-1α, to CXCR4 and subsequent signal transduction, but does not itself cause signaling and has no effect on RANTES signaling via CCR5. Thus, AMD3100 prevents CXCR4 functioning as both a HIV-1 co-receptor and a CXC-chemokine receptor. Development of small molecule inhibitors of HIV-1 entry is feasible.
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