Ningaraj N S, Salimath B P, Sankpal U T, Perera R, Vats T
Department of Pediatric Neurooncology and Molecular Pharmacology, Hoskins Center, Curtis and Elizabeth Anderson Cancer Institute, Memorial Health University Medical Center, Mercer University Medical School, 4700 Waters Avenue, Savannah, GA 31404, U.S.A.
Drug Target Insights. 2007;2:197-207. Epub 2007 Aug 17.
Brain tumor is associated with poor prognosis. The treatment option is severely limited for a patient with brain tumor, despite great advances in understanding the etiology and molecular biology of brain tumors that have lead to breakthroughs in developing pharmaceutical strategies, and ongoing NCI/Pharma-sponsored clinical trials. We reviewed the literature on molecular targeted agents in preclinical and clinical studies in brain tumor for the past decade, and observed that the molecular targeting in brain tumors is complex. This is because no single gene or protein can be affected by single molecular agent, requiring the use of combination molecular therapy with cytotoxic agents. In this review, we briefly discuss the potential molecular targets, and the challenges of targeted brain tumor treatment. For example, glial tumors are associated with over-expression of calcium-dependent potassium (K(Ca)) channels, and high grade glioma express specific K(Ca) channel gene (gBK) splice variants, and mutant epidermal growth factor receptors (EGFRvIII). These specific genes are promising targets for molecular targeted treatment in brain tumors. In addition, drugs like Avastin and Gleevec target the molecular targets such as vascular endothelial cell growth factor receptor, platelet-derived growth factor receptors, and BRC-ABL/Akt. Recent discovery of non-coding RNA, specifically microRNAs could be used as potential targeted drugs. Finally, we discuss the role of anti-cancer drug delivery to brain tumors by breaching the blood-brain tumor barrier. This non-invasive strategy is particularly useful as novel molecules and humanized monoclonal antibodies that target receptor tyrosine kinase receptors are rapidly being developed.
脑肿瘤预后较差。尽管在理解脑肿瘤的病因和分子生物学方面取得了巨大进展,这些进展已在开发药物策略方面带来突破,并且美国国立癌症研究所/制药公司正在进行临床试验,但脑肿瘤患者的治疗选择仍然极为有限。我们回顾了过去十年中关于脑肿瘤临床前和临床研究中分子靶向药物的文献,发现脑肿瘤中的分子靶向作用很复杂。这是因为没有单个基因或蛋白质能被单一分子药物所影响,需要将分子疗法与细胞毒性药物联合使用。在本综述中,我们简要讨论了潜在的分子靶点以及靶向治疗脑肿瘤所面临的挑战。例如,胶质肿瘤与钙依赖性钾(K(Ca))通道的过度表达有关,高级别胶质瘤表达特定的K(Ca)通道基因(gBK)剪接变体以及突变的表皮生长因子受体(EGFRvIII)。这些特定基因是脑肿瘤分子靶向治疗的有前景的靶点。此外,像阿瓦斯汀和格列卫这样的药物靶向血管内皮细胞生长因子受体、血小板衍生生长因子受体以及BRC-ABL/Akt等分子靶点。最近发现的非编码RNA,特别是微小RNA,可作为潜在的靶向药物。最后,我们讨论了通过突破血脑肿瘤屏障将抗癌药物递送至脑肿瘤的作用。随着针对受体酪氨酸激酶受体的新型分子和人源化单克隆抗体的快速研发,这种非侵入性策略尤为有用。