Johanssen Timothy, McVeigh Laura, Erridge Sara, Higgins Geoffrey, Straehla Joelle, Frame Margaret, Aittokallio Tero, Carragher Neil O, Ebner Daniel
Target Discovery Institute, Nuffield Department of Medicine, University of Oxford, Oxford, United Kingdom.
Cancer Research UK Scotland Centre, Institute of Genetics and Cancer, University of Edinburgh, Edinburgh, United Kingdom.
Front Oncol. 2023 Jan 17;12:1075559. doi: 10.3389/fonc.2022.1075559. eCollection 2022.
Glioblastoma (GBM) remains a cancer of high unmet clinical need. Current standard of care for GBM, consisting of maximal surgical resection, followed by ionisation radiation (IR) plus concomitant and adjuvant temozolomide (TMZ), provides less than 15-month survival benefit. Efforts by conventional drug discovery to improve overall survival have failed to overcome challenges presented by inherent tumor heterogeneity, therapeutic resistance attributed to GBM stem cells, and tumor niches supporting self-renewal. In this review we describe the steps academic researchers are taking to address these limitations in high throughput screening programs to identify novel GBM combinatorial targets. We detail how they are implementing more physiologically relevant phenotypic assays which better recapitulate key areas of disease biology coupled with more focussed libraries of small compounds, such as drug repurposing, target discovery, pharmacologically active and novel, more comprehensive anti-cancer target-annotated compound libraries. Herein, we discuss the rationale for current GBM combination trials and the need for more systematic and transparent strategies for identification, validation and prioritisation of combinations that lead to clinical trials. Finally, we make specific recommendations to the preclinical, small compound screening paradigm that could increase the likelihood of identifying tractable, combinatorial, small molecule inhibitors and better drug targets specific to GBM.
胶质母细胞瘤(GBM)仍然是一种临床需求远未得到满足的癌症。目前GBM的标准治疗方案包括最大限度的手术切除,随后进行电离辐射(IR)以及同步和辅助替莫唑胺(TMZ)治疗,其生存期获益不足15个月。传统药物研发为提高总生存期所做的努力未能克服由肿瘤固有异质性、GBM干细胞导致的治疗耐药性以及支持自我更新的肿瘤微环境所带来的挑战。在这篇综述中,我们描述了学术研究人员在高通量筛选项目中为解决这些局限性以确定新的GBM联合靶点所采取的步骤。我们详细介绍了他们如何实施更具生理相关性的表型分析,这种分析能更好地概括疾病生物学的关键领域,同时结合更具针对性的小分子化合物库,如药物再利用、靶点发现、具有药理活性的新型化合物库以及更全面的抗癌靶点注释化合物库。在此,我们讨论了当前GBM联合试验的基本原理,以及需要更系统、透明的策略来识别、验证和优先选择可进入临床试验的联合方案。最后,我们对临床前小分子筛选模式提出具体建议,这可能会增加识别出针对GBM的易处理、联合、小分子抑制剂和更好药物靶点的可能性。