选择性瘤细胞向由白素的脱糖类部分的选择性瘤细胞向
Zhiqiang Yu1, Ryan M Schmaltz, Trevor C Bozeman
1Center for BioEnergetics, Biodesign Institute, and Department of Chemistry & Biochemistry, Arizona State University, Tempe, Arizona 85287, USA.
Journal of the American Chemical Society
|February 6, 2013
概括
蓝素脱糖化合物部分对于向瘤细胞至关重要且足够,而不仅仅是针对整个蓝素分子. 这一发现是开发新的瘤成像和治疗剂的关键.
科学领域:
- 生物化学 生物化学
- 分子生物学分子生物学
- 在瘤学瘤学.
背景情况:
- 白素 (BLM) 是一种抗瘤剂,具有已知的瘤向性质.
- 之前的研究表明,BLM分糖组对于瘤选择性是必要的.
- 脱糖酸对向和其细胞吸收的充分性仍未得到证实.
研究的目的:
- 为了确定单独的白胺脱糖分量是否足以向瘤细胞.
- 为了研究白胺分糖的细胞吸收.
- 探索对新型瘤向剂设计的影响.
主要方法:
- 结合白素 (BLM),降甘素 (deglycoBLM) 和BLM分糖化物到氨酸染料Cy5**.
- 在人类乳腺 (MCF-7),前列腺 (DU-145) 和胰腺 (BxPC-3) 癌细胞系中测试这些结合物的选择性结合和内化,与它们的正常对应物一起.
- 比较BLM及其脱糖的准效率.
主要成果:
- BLM和BLM二糖化合物选择性地与MCF-7,DU-145和BxPC-3癌细胞结合并被这些癌细胞内化.
- 德格利科博莱米辛合物没有表现出选择性向.
- 脱糖的向效率与BLM在测试的癌症细胞系中相当或略低于BLM的向效率.
结论:
- 蓝素脱糖化物部分对于瘤细胞向是必要的,也是足够的.
- 这一发现对设计新瘤成像和治疗剂具有重大意义.
- 脱糖体本身可以调解选择性瘤细胞的识别和内部化.
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