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丝氨酸/苏氨酸激酶Pim-1的调节剂和抑制剂在肿瘤治疗中的应用(综述)

Use of regulators and inhibitors of Pim-1, a serine/threonine kinase, for tumour therapy (review).

作者信息

Liang Chen, Li Ying-Yi

机构信息

Department of Oncology, Cancer Research Institute, Fudan University Shanghai Cancer Center, Shanghai Medical College, Fudan University, Shanghai 200032, P.R. China.

出版信息

Mol Med Rep. 2014 Jun;9(6):2051-60. doi: 10.3892/mmr.2014.2139. Epub 2014 Apr 11.

Abstract

Pim-1 is a proto-oncogene that encodes a serine/threonine kinase that is overexpressed in a range of haematopoietic malignancies and solid cancers. Pim-1 expression is tightly regulated by multiple biomolecules at different levels. Several lines of evidence have indicated that dysregulation of Pim-1 can interfere with the cell cycle and apoptosis to promote malignant transformation of a number of types of tumour. Thus, investigation of Pim-1 regulation may provide important theoretical guidance for the development of molecular targeting therapies and drug treatments for Pim-1‑associated diseases. Regulators of Pim-1 expression, include microRNAs, oestrogen, inecalcitol, adenosine triphosphate (ATP) mimetic inhibitors and ATP competitive inhibitors of Pim-1. Combinations of inhibitors of Pim-1 expression and Pim-1‑specific inhibitors may provide novel therapies for cancer patients and directions for cancer treatment.

摘要

Pim-1是一种原癌基因,编码一种丝氨酸/苏氨酸激酶,该激酶在一系列血液系统恶性肿瘤和实体癌中过表达。Pim-1的表达在不同水平上受到多种生物分子的严格调控。多项证据表明,Pim-1的失调可干扰细胞周期和细胞凋亡,从而促进多种类型肿瘤的恶性转化。因此,研究Pim-1的调控可能为开发针对Pim-1相关疾病的分子靶向疗法和药物治疗提供重要的理论指导。Pim-1表达的调节因子包括微小RNA、雌激素、骨化二醇、三磷酸腺苷(ATP)模拟抑制剂和Pim-1的ATP竞争性抑制剂。Pim-1表达抑制剂与Pim-1特异性抑制剂的联合应用可能为癌症患者提供新的治疗方法,并为癌症治疗指明方向。

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