Belinostat (PXD101)

Belinostat (PXD101)是一种新型的和有效的羟肟酸型组蛋白去乙酰化酶（HDAC）抑制剂。在Hela细胞提取物中，belinostat抑制HDAC的活性，IC50值为27 nM。在一系列肿瘤细胞系中，belinostat显著增加组蛋白H3和H4的乙酰化，具有细胞毒性效应。在尿路上皮癌细胞系中，belinostat剂量依赖地抑制5637、T24、J82和RT4细胞的增殖，IC50值分别为1.0 μM、3.5 μM、6.0 μM和10 μM。然而，在前列腺癌细胞系中，belinostat抑制癌细胞的生长，IC50范围介于0.5-2.5 μM之间。

参考文献：
Michael T Buckley, Joanne Yoon, Herman Yee, Luis Chiriboga, Leonard Liebes, Gulshan Ara, Xiaozhong Qian, Dean F Bajorin, Tung-Tien Sun, Xue-Ru Wu and Iman Osman.  The histone deacetylase inhibitor belinostat (PXD101) suppresses bladder cancer cell growth in vitro and in vivo. Journal of Translational Medicine 2007; 5:49
Giovanni Luca Gravina, Francesco Marampon, Ilaria Giusti, Eleonora Carosa, Stefania Di Sante, Enrico Ricevuto, Vincenza Dolo, Vincenzo Tombolini, Emmanuele A Jannini and Claudio Festuccia.  Differential effects of PXD101 (belinostat) on androgen-dependent and androgen-independent prostate cancer models. International Journal of Oncology 40: 711-720, 2012
Plumb JA, Finn PW, Williams RJ, Bandara MJ, Romero MR, Watkins CJ, La Thangue NB, Brown R.  Pharmacodynamic response and inhibition of growth of human tumor xenografts by the novel histone deacetylase inhibitor PXD101. Mol Cancer Ther. 2003 Aug;2(8):721-8.