肿瘤归巢肽 iRGD 与组蛋白去乙酰化酶抑制剂丙戊酸的合成及活性
Synthesis and activity of tumor-homing peptide iRGD and histone deacetylase inhibitor valproic acid conjugate.
机构信息
Department of Pharmaceutics and Pharmaceutical Chemistry/CCCD, University of Utah, Salt Lake City, UT 84112, USA.
Department of Pharmaceutics and Pharmaceutical Chemistry/CCCD, University of Utah, Salt Lake City, UT 84112, USA; Department of Bioengineering, University of Utah, Salt Lake City, UT 84112, USA.
出版信息
Bioorg Med Chem Lett. 2014 Apr 15;24(8):1928-33. doi: 10.1016/j.bmcl.2014.03.006. Epub 2014 Mar 12.
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.
在这封信件中，我们提出了一种简洁的策略来制备肿瘤归巢肽 iRGD 和组蛋白去乙酰化酶抑制剂丙戊酸的缀合物，VPA-GFLG-iRGD。缀合物 VPA-GFLG-iRGD 和 VPA 与 GFLG-iRGD 的混合物对 DU-145 前列腺癌细胞表现出相似的细胞毒性。然而，用缀合物 VPA-GFLG-iRGD 处理 DU-145 细胞导致 G2 期细胞的百分比降低，而暴露于 VPA 和 GFLG-iRGD 的混合物导致 G2 期细胞的百分比增加。我们还发现，在测试浓度下，GFLG-iRGD 具有细胞毒性。
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