Glioblastoma: current status, emerging targets, and recent advances

A Thakur, C Faujdar, R Sharma, S Sharma… - Journal of Medicinal …, 2022 - ACS Publications
Glioblastoma (GBM) is a highly malignant brain tumor characterized by a heterogeneous
population of genetically unstable and highly infiltrative cells that are resistant to …

[HTML][HTML] ONC201 and imipridones: Anti-cancer compounds with clinical efficacy

VV Prabhu, S Morrow, AR Kawakibi, L Zhou, M Ralff… - Neoplasia, 2020 - Elsevier
ONC201 was originally discovered as TNF-Related Apoptosis Inducing Ligand (TRAIL)-
inducing compound TIC10. ONC201 appears to act as a selective antagonist of the G …

Pediatric and adult H3 K27M-mutant diffuse midline glioma treated with the selective DRD2 antagonist ONC201

AS Chi, RS Tarapore, MD Hall, N Shonka… - Journal of neuro …, 2019 - Springer
Background H3 K27M-mutant diffuse midline glioma is a fatal malignancy with no proven
medical therapies. The entity predominantly occurs in children and young adults. ONC201 is …

Aurora kinase A inhibition reverses the Warburg effect and elicits unique metabolic vulnerabilities in glioblastoma

TTT Nguyen, E Shang, C Shu, S Kim, A Mela… - Nature …, 2021 - nature.com
Aurora kinase A (AURKA) has emerged as a drug target for glioblastoma (GBM). However,
resistance to therapy remains a critical issue. By integration of transcriptome, chromatin …

Therapeutic targeting of TRAIL death receptors

F Di Cristofano, A George, V Tajiknia… - Biochemical Society …, 2023 - portlandpress.com
The discovery of tumor necrosis factor-related apoptosis-inducing ligand (TRAIL) along with
its potent and selective antitumor effects initiated a decades-long search for therapeutic …

Phase I dose escalation and expansion trial of single agent ONC201 in pediatric diffuse midline gliomas following radiotherapy

SL Gardner, RS Tarapore, J Allen… - Neuro-Oncology …, 2022 - academic.oup.com
Background ONC201, a dopamine receptor D2 (DRD2) antagonist and caseinolytic
protease P (ClpP) agonist, has induced durable tumor regressions in adults with recurrent …

Targeting mitochondria with ClpP agonists as a novel therapeutic opportunity in breast cancer

R Wedam, YE Greer, DJ Wisniewski, S Weltz, M Kundu… - Cancers, 2023 - mdpi.com
Simple Summary Mitochondria, often called “the powerhouse of the cell”, generate most of
the energy required for all cellular processes. Mitochondria also provide a platform for …

Bromodomain inhibitor jq1 induces cell cycle arrest and apoptosis of glioma stem cells through the VEGF/PI3K/AKT signaling pathway

N Wen, B Guo, H Zheng, L Xu… - International …, 2019 - spandidos-publications.com
Bromodomain and extraterminal domain proteins, especially bromodomain‑containing
protein 4 (Brd4), have recently emerged as therapeutic targets for several cancers, although …

POU2F2 regulates glycolytic reprogramming and glioblastoma progression via PDPK1-dependent activation of PI3K/AKT/mTOR pathway

R Yang, M Wang, G Zhang, Y Li, L Wang, H Cui - Cell death & disease, 2021 - nature.com
Abstract The POU Class Homeobox 2 (POU2F2) is a member of POU transcription factors
family, which involves in cell immune response by regulating B cell proliferation and …

Biological activity of weekly ONC201 in adult recurrent glioblastoma patients

I Arrillaga-Romany, Y Odia, VV Prabhu… - Neuro …, 2020 - academic.oup.com
Background ONC201 is a dopamine receptor D2 (DRD2) antagonist that penetrates the
blood–brain barrier. ONC201 efficacy has been shown in glioblastoma animal models and …