Jayaraman Padma-Sheela, Gaston Kevin
Biodiscovery Institute, University of Nottingham, NG7 2UH, UK.
Division of Translational Medical Sciences, School of Medicine, University of Nottingham, NG7 2UH, UK.
Explor Target Antitumor Ther. 2021;2(5):434-447. doi: 10.37349/etat.2021.00055. Epub 2021 Oct 31.
Cholangiocarcinoma (CCA) is a disease with a very poor prognosis and limited treatment options. Although targeted therapies directed towards specific mutations found in CCA are becoming available and are showing great potential, many tumors do not carry actionable mutations and, in those that do, the emergence of drug resistance is a likely consequence of treatment. Therapeutic targeting of enzymes and other proteins that show elevated activity in CCA cells but which are not altered by mutation is a potential strategy for the treatment of target negative and drug-resistant disease. Protein kinase CK2 (CK2) is a ubiquitously expressed kinase that has increased expression and increased activity in a variety of cancer types including CCA. Several potent CK2 inhibitors are in pre-clinical development or under assessment in a variety of clinical trials often in combination with drugs that induce DNA damage. This review outlines the importance of CK2 in CCA and assesses the progress that has been made in the evaluation of CK2 inhibition as a treatment strategy in this disease. Targeting CK2 based on the expression levels or activity of this protein and/or in combination with drugs that induce DNA damage or inhibit cell cycle progression, could be a viable option for tumors that lack actionable mutations, or for tumors that develop resistance to targeted treatments.
胆管癌(CCA)是一种预后极差且治疗选择有限的疾病。尽管针对CCA中发现的特定突变的靶向治疗药物已逐渐问世并显示出巨大潜力,但许多肿瘤并不携带可用于治疗的突变,而且在那些携带此类突变的肿瘤中,耐药性的出现很可能是治疗的结果。对CCA细胞中活性升高但未发生突变的酶和其他蛋白质进行治疗性靶向,是治疗无靶向治疗靶点及耐药疾病的一种潜在策略。蛋白激酶CK2(CK2)是一种广泛表达的激酶,在包括CCA在内的多种癌症类型中表达增加且活性增强。几种有效的CK2抑制剂正处于临床前开发阶段,或正在各种临床试验中进行评估,这些试验通常与诱导DNA损伤的药物联合使用。本综述概述了CK2在CCA中的重要性,并评估了将抑制CK2作为该疾病治疗策略的评估进展。对于缺乏可用于治疗的突变的肿瘤,或对靶向治疗产生耐药性的肿瘤,基于该蛋白的表达水平或活性靶向CK2,和/或与诱导DNA损伤或抑制细胞周期进程的药物联合使用,可能是一种可行的选择。