IL4RPep-1 acetate is an interleukin-4 receptor ( IL-4R ) binding agent. IL4RPep-1 acetate preferentially binds to cells with high levels of IL-4R expression compared to those with low levels of expression. IL4RPep-1 acetate-labeled liposomes containing Doxorubicin are internalized by cells more efficiently. IL4RPep-1 acetate-labeled liposomes accumulate more effectively within H226 tumors [1].
In Vivo, IL4RPep-1 acetate-labeled doxorubicin-loaded liposomes (doxorubicin equivalent dose of 1 mg/kg; intravenous injection; twice weekly for a total of 7 times) significantly inhibit the growth of H226 lung cancer xenografts compared with the untreated control group, free doxorubicin and unlabeled liposomes, with no significant effect on mouse body weight[1].
In Vitro, IL4RPep-1 (biotin-labeled IL4RPep-1; 1-80 μM; 1 h) acetate binds to H226 squamous cell lung cancer cells with high IL-4R expression, with a dissociation constant Kd of 6.5 μM, and its binding affinity is significantly higher than that to H460 large cell lung cancer cells with low IL-4R expression (Kd = 51.9 μM)[1]. IL4RPep-1 (100 μg IL4RPep-1; 0-24 h) acetate remains stable in mouse serum at 37 °C for at least 4 h, and most of the peptide stays intact even after 24 h of incubation[1]. IL4RPep-1 (10 μM; 1 h) acetate preferentially binds to TNF-α-activated HUVEC with upregulated IL-4R expression, compared with untreated human umbilical vein endothelial cells (HUVEC)[1].
References:
[1]. Chi L, et al. Enhanced delivery of liposomes to lung tumor through targeting interleukin-4 receptor on both tumor cells and tumor endothelial cells. J Control Release. 2015;209:327-336.
In Vivo, IL4RPep-1 acetate-labeled doxorubicin-loaded liposomes (doxorubicin equivalent dose of 1 mg/kg; intravenous injection; twice weekly for a total of 7 times) significantly inhibit the growth of H226 lung cancer xenografts compared with the untreated control group, free doxorubicin and unlabeled liposomes, with no significant effect on mouse body weight[1].
In Vitro, IL4RPep-1 (biotin-labeled IL4RPep-1; 1-80 μM; 1 h) acetate binds to H226 squamous cell lung cancer cells with high IL-4R expression, with a dissociation constant Kd of 6.5 μM, and its binding affinity is significantly higher than that to H460 large cell lung cancer cells with low IL-4R expression (Kd = 51.9 μM)[1]. IL4RPep-1 (100 μg IL4RPep-1; 0-24 h) acetate remains stable in mouse serum at 37 °C for at least 4 h, and most of the peptide stays intact even after 24 h of incubation[1]. IL4RPep-1 (10 μM; 1 h) acetate preferentially binds to TNF-α-activated HUVEC with upregulated IL-4R expression, compared with untreated human umbilical vein endothelial cells (HUVEC)[1].
References:
[1]. Chi L, et al. Enhanced delivery of liposomes to lung tumor through targeting interleukin-4 receptor on both tumor cells and tumor endothelial cells. J Control Release. 2015;209:327-336.