CD4 mimetic (IC50
values are in low micromolar range, dependent on cell type and HIV strain). Recognizes and induces structural changes in HIV-1 envelope protein gp120, analogous to CD4 binding. Inhibits HIV-1 cell entry in CXCR4 and CCR5 expressing cell lines, by blocking virus-cell and cell-cell fusion.
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All Tocris products are intended for laboratory research use only.
Identification of N-phenyl-N'-(2,2,6,6-tetramethyl-piperidin-4-yl)-oxalamides as a new class of HIV-1 entry inhibitors that prevent gp120 binding to CD4.
Zhao et al.
Unliganded HIV-1 gp120 core structures assume the CD4-bound conformation with regulation by quaternary interactions and variable loops.
Kwon et al.
Peptides from second extracellular loop of C-C chemokine receptor type 5 (CCR5) inhibit diverse strains of HIV-1.
Dogo-Isonagie et al.