Figure 3
α4β1-specific binding of THI0567-targeted liposomes. (A) THI0565 competition with THI0567-targeted liposome (150 nm; 0.05% or 1.0% targeting conjugate; used at a particle concentration of 2 × 10−10 M). Average %inhibition ± SEM (n = 3 experiments). (B) Binding of THI0567-targeted liposome (2 × 10−10 M) to wildtype Jurkat cells and α4β1neg Jurkat cells (C) Binding of THI0567-targeted liposome (2 × 10−10 M) to wildtype K562 cells and a K562 cells stably expressing integrin α4β1 (α4β1pos). (D,E) THI0567-targeted liposome (150 nm; 1.0% targeting conjugate) and non-targeted liposome (150 nm; 0% targeting conjugate) binding to Jurkat and murine 70Z3 cells. In (B–E), average gMFI ± SEM (n = 3 experiments). (F) THI0567-targeted liposome binding to murine 70Z3 cells in the presence of anti-α4 mAb PS/2 or IgG2b isotype control (average gMFI ± SEM [n = 4 experiments]). (G) THI0567-targeted (Dual-Gd567) liposomes (2 × 10−10 M) were incubated with THP-1 or Jurkat T cells (1 h at RT, ± 20 mM EDTA), followed by counter-staining for FcγRI (green, THP-1) and CD3 (green, Jurkat). Blue; Hoechst 33342.
