Kuzelová Katerina, Hrkal Zbynēk
Department of Cellular Biochemistry, Institute of Hematology and Blood Transfusion, U Nemocnice 1, 128 20 Prague-2, Czech Republic.
Cardiovasc Hematol Disord Drug Targets. 2008 Dec;8(4):261-7. doi: 10.2174/187152908786786241.
Chronic myelogenous leukemia (CML) is a hematological malignancy that is characteristic by as expansion of myeloid cells and their premature release into the circulation. The molecular cause of CML is the fusion oncoprotein Bcr-Abl whose constitutive tyrosine-kinase (TK) activity maintains enhanced signaling through multiple signal transduction pathways and confers proliferative and survival advantage to CML cells. These effects can be largely suppressed by TK inhibitor Imatinib mesylate, currently the leading drug in CML treatment. However, Bcr-Abl contains also additional functional domains, in particular a DBL homology (DH) domain with guanine-exchange function (GEF) which can activate small GTPases of Rho family and a Src-homology3 (SH3) domain which recruits other proteins with GEF activity. Bcr-Abl affects among others the RhoA/ROCK/LIM/cofilin pathway that regulates the actin cytoskeleton assembly and thereby the cellular adhesion and migration. This review deals in detail with the known points of interference between Bcr-Abl and Rho kinase pathways and with the effects of Imatinib mesylate on Rho signaling and cell adhesion to the extracellular matrix (ECM) components. The potential protein targets related to Bcr-Abl non-kinase activity are discussed.
慢性粒细胞白血病(CML)是一种血液系统恶性肿瘤,其特征是髓系细胞扩增并过早释放到循环中。CML的分子病因是融合癌蛋白Bcr-Abl,其组成型酪氨酸激酶(TK)活性通过多种信号转导途径维持增强的信号传导,并赋予CML细胞增殖和生存优势。这些效应在很大程度上可被TK抑制剂甲磺酸伊马替尼抑制,甲磺酸伊马替尼是目前CML治疗的主要药物。然而,Bcr-Abl还包含其他功能域,特别是具有鸟嘌呤交换功能(GEF)的DBL同源(DH)域,其可激活Rho家族的小GTP酶,以及募集具有GEF活性的其他蛋白质的Src同源3(SH3)域。Bcr-Abl尤其影响调节肌动蛋白细胞骨架组装从而影响细胞黏附和迁移的RhoA/ROCK/LIM/丝切蛋白途径。本综述详细探讨了Bcr-Abl与Rho激酶途径之间已知的干扰点,以及甲磺酸伊马替尼对Rho信号传导和细胞与细胞外基质(ECM)成分黏附的影响。还讨论了与Bcr-Abl非激酶活性相关的潜在蛋白质靶点。