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前列腺肿瘤特异性肽-类肽杂合前药

Prostate tumor specific peptide-peptoid hybrid prodrugs.

作者信息

Lee Jiyoun, Huang Wei, Broering James M, Barron Annelise E, Seo Jiwon

机构信息

Department of Global Medical Science, Sungshin University, Seoul 142-732, Republic of Korea.

Department of Bioengineering, Stanford University, Palo Alto, CA 94305, USA.

出版信息

Bioorg Med Chem Lett. 2015 Jul 15;25(14):2849-52. doi: 10.1016/j.bmcl.2015.04.092. Epub 2015 May 6.

Abstract

Inspired by naturally occurring host defense peptides, cationic amphipathic peptoids provide a promising scaffold for anti-cancer therapeutics. Herein, we report a library of peptide-peptoid hybrid prodrugs that can be selectively activated by prostate cancer cells. We have identified several compounds demonstrating potent anti-cancer activity with good to moderate selectivity. We believe that these prodrugs can provide a useful design principle for next generation peptide-peptoid hybrid prodrugs.

摘要

受天然存在的宿主防御肽启发,阳离子两亲性类肽为抗癌治疗提供了一个有前景的支架。在此,我们报告了一个可被前列腺癌细胞选择性激活的肽-类肽杂合前药库。我们已鉴定出几种表现出强效抗癌活性且具有良好至中等选择性的化合物。我们相信这些前药可为下一代肽-类肽杂合前药提供有用的设计原则。

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