AMD070 (AMD11070) is an orally active, reversible and selective CXCR4 (CD184, fusin) antagonist (IC50 = 13 nM against 100 pM 125I-SDF-1α for binding human CD+/CXCR4+ CEM-CCRF cells) that inhibits HIV-1 replication in cultures (IC50/host cells = 2 nM/MT-4 and 26 nM/PBMCs; T-tropic HIV-1NL4.3 strain) with no host cytotoxicity even at concentrations above 23 μM.
Orally active, reversible and selective CXCR4 (CD184, fusin) antagonist that inhibits HIV-1 replication in host cell cultures.
Journal of medicinal chemistry, 53(8), 3376-3388 (2010-03-20)
The redesign of azamacrocyclic CXCR4 chemokine receptor antagonists resulted in the discovery of novel, small molecule, orally bioavailable compounds that retained T-tropic (CXCR4 using, X4) anti-HIV-1 activity. A structure-activity relationship (SAR) was determined on the basis of the inhibition of
Currently, there is no cure for Alzheimer's disease (AD). Therapeutics that can modify the early stage of AD are urgently needed. Recent studies have shown that the pathogenesis of AD is closely regulated by an endo/lysosomal asparaginyl endopeptidase (AEP). Inhibition
Netrin-1, a family member of laminin-related secreted proteins, mediates axon guidance and cell migration during neural development. T835M mutation in netrin receptor UNC5C predisposes to the late-onset Alzheimer's disease (AD) and increases neuronal cell death. However, it remains unclear how
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