Synthesis and activity of tumor-homing peptide iRGD and histone deacetylase inhibitor valproic acid conjugate

被引：12

作者：

Peng, Zheng-Hong ^{[1
]}

Kopecek, Jindrich ^{[1
,2
]}

机构：

[1] Univ Utah, Dept Pharmaceut & Pharmaceut Chem, CCCD, Salt Lake City, UT 84112 USA

[2] Univ Utah, Dept Bioengn, Salt Lake City, UT 84112 USA

来源：

BIOORGANIC & MEDICINAL CHEMISTRY LETTERS | 2014年 / 24卷 / 08期

基金：

美国国家卫生研究院;

关键词：

Histone deacetylase inhibitor; Valproic acid; Cell penetrating peptide; Cell cycle arrest; PROSTATE-CANCER CELLS; PENETRATING PEPTIDE; IN-VITRO; DELIVERY; EXPRESSION; INTEGRINS; EFFICACY; DESIGN; DRUGS; VIVO;

D O I：

10.1016/j.bmcl.2014.03.006

中图分类号：

R914 [药物化学];

学科分类号：

100701 ;

摘要：

In this Letter, we present a concise strategy to prepare a conjugate of the tumor homing peptide iRGD and histone deacetylase inhibitor valproic acid, VPA-GFLG-iRGD. The conjugate VPA-GFLG-iRGD and a mixture of VPA and GFLG-iRGD have shown similar cytotoxicity against DU-145 prostate cancer cells. However, the treatment of DU-145 cells with conjugate VPA-GFLG-iRGD resulted in a decreased percentage of cells in the G2 phase, whereas the exposure of a mixture of VPA and GFLG-iRGD led to an increased percentage of cells in the G2 phase. We also found that GFLG-iRGD possessed cytotoxicity at the tested concentrations. (C) 2014 Elsevier Ltd. All rights reserved.

引用

页码：1928 / 1933

页数：6

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