Department of Hematology and Bone Marrow Transplantation, Chaim Sheba Medical Center, The Guy Weinshtock Multiple Myeloma Foundation, Tel-Hashomer, Israel.
PLoS One. 2012;7(4):e33856. doi: 10.1371/journal.pone.0033856. Epub 2012 Apr 25.
Multiple Myeloma (MM) is a lymphatic neoplasm characterized by clonal proliferation of malignant plasma cell that eventually develops resistance to chemotherapy. Drug resistance, differentiation block and increased survival of the MM tumor cells result from high genomic instability. Chromosomal translocations, the most common genomic alterations in MM, lead to dysregulation of cyclin D, a regulatory protein that governs the activation of key cell cycle regulator--cyclin dependent kinase (CDK). Genomic instability was reported to be affected by over expression of another CDK regulator--cyclin E (CCNE). This occurs early in tumorigenesis in various lymphatic malignancies including CLL, NHL and HL. We therefore sought to investigate the role of cyclin E in MM. CCNE1 expression was found to be heterogeneous in various MM cell lines (hMMCLs). Incubation of hMMCLs with seliciclib, a selective CDK-inhibitor, results in apoptosis which is accompanied by down regulation of MCL1 and p27. Ectopic over expression of CCNE1 resulted in reduced sensitivity of the MM tumor cells in comparison to the paternal cell line, whereas CCNE1 silencing with siRNA increased the cell sensitivity to seliciclib. Adhesion to FN of hMMCLs was prevented by seliciclib, eliminating adhesion-mediated drug resistance of MM cells. Combination of seliciclib with flavopiridol effectively reduced CCNE1 and CCND1 protein levels, increased subG1 apoptotic fraction and promoted MM cell death in BMSCs co-culture conditions, therefore over-coming stroma-mediated protection. We suggest that seliciclib may be considered as essential component of modern anti MM drug combination therapy.
多发性骨髓瘤(MM)是一种淋巴肿瘤,其特征是恶性浆细胞的克隆性增殖,最终对化疗产生耐药性。耐药性、分化阻滞和 MM 肿瘤细胞的存活增加是由于基因组高度不稳定所致。染色体易位是 MM 中最常见的基因组改变,导致调节蛋白细胞周期蛋白 D 的失调,细胞周期蛋白 D 调节关键细胞周期调节剂——细胞周期蛋白依赖性激酶(CDK)的激活。据报道,基因组不稳定性受另一种 CDK 调节因子——细胞周期蛋白 E(CCNE)的过度表达影响。这种情况发生在包括 CLL、NHL 和 HL 在内的各种淋巴恶性肿瘤的早期肿瘤发生过程中。因此,我们试图研究细胞周期蛋白 E 在 MM 中的作用。在各种 MM 细胞系(hMMCLs)中发现 CCNE1 表达存在异质性。用选择性 CDK 抑制剂 seliciclib 孵育 hMMCLs 会导致细胞凋亡,同时下调 MCL1 和 p27。与亲代细胞系相比,CCNE1 的异位过表达导致 MM 肿瘤细胞对 seliciclib 的敏感性降低,而用 siRNA 沉默 CCNE1 则增加了细胞对 seliciclib 的敏感性。seliciclib 可阻止 hMMCLs 与 FN 的黏附,消除 MM 细胞的黏附介导的耐药性。seliciclib 与 flavopiridol 的联合使用可有效降低 CCNE1 和 CCND1 蛋白水平,增加 subG1 凋亡分数,并在 BMSCs 共培养条件下促进 MM 细胞死亡,从而克服基质介导的保护作用。我们认为 seliciclib 可被视为现代抗 MM 药物联合治疗的重要组成部分。