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.
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http://dx.doi.org/10.3389/fonc.2022.1075559 | DOI Listing |
Eur J Pharmacol
December 2024
The School of Biomedical and Pharmaceutical Sciences, Guangdong University of Technology, Guangzhou, 510006, PR China. Electronic address:
Glioblastoma multiforme (GBM) is a highly heterogeneous and aggressive brain tumor, which presents significant challenges for treatment in clinical settings. Phosphodiesterase 4 (PDE4) inhibitors can prevent the degradation of cAMP and have been used as a potential targeted therapeutic approach for different cancer types. However, its clinical use is restricted by the side effects such as nausea and vomiting.
View Article and Find Full Text PDFBiomaterials
December 2024
Department of Neurosurgery, Yale University, New Haven, CT, 06511, USA; Department of Biomedical Engineering, Yale University, New Haven, CT, 06510, USA. Electronic address:
Glioblastoma (GBM), the most common primary brain tumor, lacks effective treatments. Emerging evidence suggests mitochondria as a promising therapeutic target, albeit successfully targeting represents a major challenge. Recently, we discovered a group of triterpenes that can self-assemble into nanoparticles (NPs) for cancer treatment.
View Article and Find Full Text PDFNeuro Oncol
December 2024
Department of Neurosurgery, Xiangya Hospital, Central South University, Changsha, Hunan, China.
Background: Selinexor is a selective inhibitor of exportin-1 (XPO1), a key mediator of the nucleocytoplasmic transport for molecules critical to tumor cell survival. Selinexor's lethality is generally associated with the induction of apoptosis, and in some cases, with autophagy-induced apoptosis. We performed this study to determine Selinexor's action in glioblastoma (GBM) cells, which are notoriously resistant to apoptosis.
View Article and Find Full Text PDFJ Nanobiotechnology
December 2024
Key Laboratory of Emergency and Trauma of Ministry of Education, Engineering Research Center for Hainan Biological Sample Resources of Major Diseases, the Hainan Branch of National Clinical Research Center for Cancer, the First Affiliated Hospital, Hainan Medical University, Haikou, 570102, China.
Limited drug accumulation and an immunosuppressive microenvironment are the major bottlenecks in the treatment of glioblastoma multiforme (GBM). Herein, we report a copper-coordination driven brain-targeting nanoassembly (TCe6@Cu/TP5 NPs) for site-specific delivery of therapeutic agents and efficient immunotherapy by activating the cGAS-STING pathway and downregulating the expression of PD-L1. To achieve this, the mitochondria-targeting triphenylphosphorus (TPP) was linked to photosensitizer Chlorin e6 (Ce6) to form TPP-Ce6 (TCe6), which was then self-assembled with copper ions and thymopentin (TP5) to obtain TCe6@Cu/TP5 NPs.
View Article and Find Full Text PDFBMC Cancer
December 2024
Department of Data Science, Faculty of Interdisciplinary Science and Technology, Tarbiat Modares University, Tehran, Iran.
Glioblastoma Multiforme (GBM), classified as a grade IV glioma by the World Health Organization (WHO), is a prevalent and notably aggressive form of brain tumor derived from glial cells. It stands as one of the most severe forms of primary brain cancer in humans. The median survival time of GBM patients is only 12-15 months, making it the most lethal type of brain tumor.
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