Laboratório de Bioquímica e Biofísica, Instituto Butantan, Av. Vital Brazil 1500, 05503-900, São Paulo SP, Brazil.
Toxicon. 2010 Dec 15;56(7):1145-54. doi: 10.1016/j.toxicon.2010.04.019. Epub 2010 May 31.
The aim of this study was to evaluate the anti-tumor activity of Amblyomin-X, a serine protease Kunitz-type inhibitor. Amblyomin-X induced tumor mass regression and decreased number of metastatic events in a B16F10 murine melanoma model. Alterations on expression of several genes related to cell cycle were observed when two tumor cell lines were treated with Amblyomin-X. PSMB2, which encodes a proteasome subunit, was differentially expressed, in agreement to inhibition of proteasomal activity in both cell lines. In conclusion, our results indicate that Amblyomin-X selectively acts on tumor cells by inducing apoptotic cell death, possibly by targeting the ubiquitin-proteasome system.
本研究旨在评估 Amblyomin-X（一种丝氨酸蛋白酶 Kunitz 型抑制剂）的抗肿瘤活性。Amblyomin-X 诱导 B16F10 鼠黑色素瘤模型中的肿瘤质量消退，并减少转移事件的数量。当两种肿瘤细胞系用 Amblyomin-X 处理时，观察到与细胞周期相关的几个基因的表达发生改变。PSMB2 编码蛋白酶体亚基，其表达水平不同，这与两种细胞系中蛋白酶体活性的抑制一致。总之，我们的结果表明，Amblyomin-X 通过诱导细胞凋亡选择性地作用于肿瘤细胞，可能通过靶向泛素-蛋白酶体系统。
