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

BIOORGANIC & MEDICINAL CHEMISTRY LETTERS

卷:24

Article

Peng, Zheng-Hong¹  Kopecek, Jindrich^1,2 

[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

关键词: Histone deacetylase inhibitor;    Valproic acid;    Cell penetrating peptide;    Cell cycle arrest;   

DOI  :  10.1016/j.bmcl.2014.03.006

来源: Elsevier

【 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.

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