Title: AMD3100, a small molecule inhibitor of HIV-1 entry via the CXCR4 co-receptor
Authors: Donzella, G A ×
Schols, Dominique
Lin, S W
Esté, J A
Nagashima, K A
Maddon, P J
Allaway, G P
Sakmar, T P
Henson, G
De Clercq, Erik
Moore, J P #
Issue Date: Jan-1998
Series Title: Nature medicine vol:4 issue:1 pages:72-7
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-1alpha, 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.
ISSN: 1078-8956
Publication status: published
KU Leuven publication type: IT
Appears in Collections:Laboratory of Virology and Chemotherapy (Rega Institute)
× corresponding author
# (joint) last author

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