11月22日,，日本濱松醫(yī)科大學(xué)的一個(gè)研究小組公布，他們開發(fā)出一種可減輕副作用的抗癌劑,，通過動(dòng)物實(shí)驗(yàn)發(fā)現(xiàn)效果顯著,。
惡性腫瘤在成長到1至2厘米以上大小時(shí)，就會生長出吸收營養(yǎng)的“新生血管”,。杉原一廣準(zhǔn)教授領(lǐng)導(dǎo)的研究小組發(fā)現(xiàn),，連接氨基酸的一種肽具有易于在新生血管積聚的特性。他們據(jù)此開發(fā)出與肽組合的抗癌藥物,，這種抗癌藥物僅對新生血管起作用,。
濱松醫(yī)科大學(xué)與美國桑福德伯納姆醫(yī)學(xué)研究所共同開展實(shí)驗(yàn)，把該抗癌藥物投給患有癌癥的小鼠,。結(jié)果發(fā)現(xiàn)，僅用過去用藥量的四十分之一,，在19天之內(nèi)癌細(xì)胞消失,，而小鼠完全沒有出現(xiàn)副作用。研究小組計(jì)劃對該藥物進(jìn)行臨床試驗(yàn),，爭取早日實(shí)現(xiàn)應(yīng)用,。
該研究成果發(fā)表于美國《國家科學(xué)院院刊》（PNAS）電子版。(生物谷Bioon.com)
doi:10.1073/pnas.1105057108
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PMID:
Targeted drug delivery to tumor vasculature by a carbohydrate mimetic peptide
Hatakeyama, Shingo; Sugihara, Kazuhiro; Shibata, Toshiaki K.; Nakayama, Jun; Akama, Tomoya O.; Tamura, Naoaki; Wong, Shuk-Man; Bobkov, et al.
Although numerous carbohydrates play significant roles in mammalian cells, carbohydrate-based drug discovery has not been explored due to the technical difficulty of chemically synthesizing complex carbohydrate structures. Previously, we identified a series of carbohydrate mimetic peptides and found that a 7-mer peptide, designated I-peptide, inhibits hematogenous carbohydrate-dependent cancer cell colonization. During analysis of the endothelial surface receptor for I-peptide, we found that I-peptide bound to annexin 1 (Anxa1). Because Anxa1 is a highly specific tumor vasculature surface marker, we hypothesized that an I-peptide-like peptide could target anticancer drugs to the tumor vasculature. This study identifies IFLLWQR peptide, designated IF7, as homing to tumors. When synthetic IF7 peptide was conjugated to fluorescent Alexa 488 (A488) and injected intravenously into tumor-bearing mice, IF7-A488 targeted tumors within minutes. IF7 conjugated to the potent anticancer drug SN-38 and injected intravenously into nude mice carrying human colon HCT116 tumors efficiently suppressed tumor growth at low dosages with no apparent side effects. These results suggest that IF7 serves as an efficient drug delivery vehicle by targeting Anxa1 expressed on the surface of tumor vasculature. Given its extremely specific tumor-targeting activity, IF7 may represent a clinically relevant vehicle for anticancer drugs.
