AMD3100, a small molecule inhibitor of HIV-1 entry via the CXCR4 co-receptor

被引：0
|
作者：
George A. Donzella
Dominique Schols
Steven W. Lin
José A. Esté
Kirsten A. Nagashima
Paul J. Maddon
Graham P. Allaway
Thomas P. Sakmar
Geoffrey Henson
Erik DeClercq
John P. Moore
机构：
[1] The Rockefeller University,The Aaron Diamond AIDS Research Center
[2] Katholieke Universiteit,Rega Institute for Medical Research
[3] Howard Hughes Medical Institute,undefined
[4] The Rockefeller University,undefined
[5] Progenics Pharmaceuticals,undefined
[6] AnorMED,undefined
来源：
Nature Medicine | 1998年 / 4卷
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摘要：
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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页码：72 / 77
页数：5
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