Determinants for Sensitivity of Human Immunodeficiency Virus Coreceptor CXCR4 to the Bicyclam AMD3100
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چکیده
منابع مشابه
Determinants for sensitivity of human immunodeficiency virus coreceptor CXCR4 to the bicyclam AMD3100.
The bicyclam AMD3100 is a potent and selective inhibitor of the replication of human immunodeficiency virus type 1 and type 2 (HIV-1 and HIV-2). It was recently demonstrated that the compound inhibited HIV entry through CXCR4 but not through CCR5. Selectivity of AMD3100 for CXCR4 was further indicated by its lack of effect on HIV-1 and HIV-2 infection mediated by the CCR5, CCR3, Bonzo, BOB, and...
متن کاملMutation of Asp and Asp of the Chemokine Receptor CXCR4 Impairs Its Coreceptor Function for Human Immunodeficiency Virus-1 Entry and Abrogates the Antagonistic Activity of AMD3100
The bicyclam AMD3100 is a highly potent and selective CXCR4 antagonist with strong antiviral activity against human immunodeficiency virus (HIV)-1 and HIV-2, which use CXCR4 as coreceptor for host cell entry. Here, we investigated the interaction of AMD3100 with CXCR4 at the molecular level by mutational analysis. We established a set of stably transfected U87.CD4 cell lines expressing differen...
متن کاملCXCR4 as a functional coreceptor for human immunodeficiency virus type 1 infection of primary macrophages.
The coreceptors used by primary syncytium-inducing (SI) human immunodeficiency virus type 1 isolates for infection of primary macrophages were investigated. SI strains using only CXCR4 replicated equally well in macrophages with or without CCR5 and were inhibited by several different ligands for CXCR4 including SDF-1 and bicyclam derivative AMD3100. SI strains that used a broad range of corecep...
متن کاملActivity of different bicyclam derivatives against human immunodeficiency virus depends on their interaction with the CXCR4 chemokine receptor.
Bicyclams represent a novel class of selective anti-HIV inhibitors with potent activity against T-cell tropic strains of HIV. The prototype compound, the bicyclam AMD3100, has an EC50 of 1 to 10 ng/ml against different strains of HIV-1, including clinical isolates. AMD3100 was shown to interact with the CXC-chemokine receptor CXCR4, the main coreceptor used by T-cell tropic strains of HIV. Here...
متن کاملInhibition of HIV infection by bicyclams, highly potent and specific CXCR4 antagonists.
The bicyclams represent a new entity of low-molecular weight molecules that inhibit human immunodeficiency virus (HIV) infection through a specific blockade of CXCR4 (fusin), the receptor for the CXC chemokine SDF-1 (soluble-derived factor), which is also used as coreceptor by T-lymphotropic HIV strains to enter their target cells. The bicyclam AMD3100 or 1,1'-[1,4-phenylenebis(methylene)]-bis-...
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ژورنال
عنوان ژورنال: Journal of Virology
سال: 1998
ISSN: 0022-538X,1098-5514
DOI: 10.1128/jvi.72.8.6381-6388.1998