很多抗癌藥物由于血腦屏障的限制對(duì)腦瘤作用比較差，不利于藥物的吸收。紫杉醇是二萜類天然產(chǎn)物，其在體外能有效地抑制惡性腦膠質(zhì)瘤的生長(zhǎng)，但并不能顯著提高惡性腦膠質(zhì)瘤患者存活時(shí)間，其原因主要是紫杉醇在血漿中消除太快，血腦屏障滲透能力差等導(dǎo)致腫瘤部位吸收過(guò)低。為了解決這個(gè)問(wèn)題，一種可靶向低密度脂蛋白受體相關(guān)蛋白-1（LRP-1）的19個(gè)氨基酸的肽Angiopep-2與3分子紫杉醇結(jié)合構(gòu)成ANG1005，ANG1005與LRP-1結(jié)合作用后可以促使受體介導(dǎo)的藥物通過(guò)跨細(xì)胞轉(zhuǎn)運(yùn)進(jìn)入腦組織中。

Owing to the limit of the blood-brain barrier (BBB) many anticancer drugs have undesirable effect on brain tumors with less benefit for drug absorption. Paclitaxel, a natural product belonging to diterpene, could effectively inhibit the growth of malignant glioma and brain metastases in vitro. However it could not significantly improve survival time of patient suffered from malignant glioma. The main reason is that paciltaxel is eliminated too fast in the plasma and the BBB penetration ability is too low causing lower absorption at tumor sites. To overcome this problem, a targeted low-density lipoprotein (LDL) receptor-related protein-1 (LRP-1) of 19-amino acid peptide Angiopep-2 and three molecular paclitaxel constitute ANG1005. After combination of ANG1005 and LRP-1, receptor-mediated drugs could be promoted to brain tissue through cell transportation.