Calandrella N, Risuleo G, Scarsella G, Mustazza C, Castelli M, Galati F, Giuliani A, Galati G
Department of Cell Biology and Development, University of Rome La Sapienza, Italy.
J Exp Clin Cancer Res. 2007 Sep;26(3):405-9.
Cell proliferation control plays a key role in tumor development. The basic Fibroblast Growth Factor (bFGF), as well as other growth factors, is involved in several pathologies characterized by dysregulation of cell proliferation. In the present work the effects of PD166866, a very potent and selective tyrosine kinase inhibitor were evaluated. Cultured murine fibroblasts (the cell line 3T6) were used to assess the FGFR-1 inhibition mediated by PD166866. Evaluation of cell viability and molecular biology techniques were adopted. PD166866 controls negatively the bFGF/FGFR-1 system thus promoting a significant reduction of cell proliferation and loss of viability in 3T6 cells. The drug possibly controls proliferation via induction of apoptosis as evidenced by a relevant chromatin degradation.
This study demonstrated that PD166866 might be used in the control of fibrotic proliferative diseases, as well as in other tumor pathologies.
细胞增殖控制在肿瘤发展中起关键作用。碱性成纤维细胞生长因子（bFGF）以及其他生长因子参与了几种以细胞增殖失调为特征的病理过程。在本研究中，评估了一种非常强效且选择性的酪氨酸激酶抑制剂PD166866的作用。使用培养的小鼠成纤维细胞（3T6细胞系）来评估PD166866介导的FGFR-1抑制作用。采用了细胞活力评估和分子生物学技术。PD166866对bFGF/FGFR-1系统具有负向调控作用，从而显著促进3T6细胞的细胞增殖减少和活力丧失。该药物可能通过诱导凋亡来控制增殖，相关染色质降解证明了这一点。
本研究表明，PD166866可用于控制纤维化增殖性疾病以及其他肿瘤病理。
