Development of intelligent-type drug delivery system by transporter protein.

我们构建了NGR（Asn-Gly-Arg）-lipocalin-type prostaglandin D synthase（L-PGDS），具有肿瘤靶向性NGR基序，能特异性结合血管内皮细胞表达的CD 13受体。NGR-L-PGDS与水溶性差的抗肿瘤药物SN-38复合。与在PBS中的溶解度相比，在PBS中存在2 mM NGR-L-PGDS的情况下SN-38的溶解度增加了300倍。在使用人结肠癌细胞的小鼠异种移植肿瘤模型中，与对照相比，SN-38/NGR-L-PGDS复合物静脉给药显著抑制肿瘤生长。

We generated NGR (Asn-Gly-Arg)-lipocalin-type prostaglandin D synthase (L-PGDS), possessing tumor-targeting NGR-motif, which specifically binds to CD13 receptor expressing in the endothelium of angiogenic blood vessels. NGR-L-PGDS was complexed with SN-38 which is a poorly water-soluble antitumor drug. The solubility of SN-38 in the presence of 2 mM NGR-L-PGDS in PBS increased by 300-fold as compared with that in PBS. Intravenous administration of SN-38/NGR-L-PGDS complex dominantly inhibited tumor growth as compared with control in mouse xenograft tumor model using human colon cancer cells.