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Integrated screening for small molecules interfering with PKM2: a drug repurposing strategy against glioblastoma.


ABSTRACT:

Background

Glioblastoma (GBM), the most aggressive adult brain tumor, remains a significant clinical challenge. Pyruvate kinase M2 (PKM2), by shifting between its tetrameric (metabolic) and dimeric (oncogenic) forms, drives GBM metabolism and tumorigenesis, regulating the Warburg effect. This study explores a drug repurposing strategy to identify clinically approved medications capable of stabilizing PKM2 in its tetrameric form, thus disrupting GBM metabolic adaptability and oncogenic potential.

Methods

We employed a multi-step screening strategy that integrates virtual screening, pharmacological data analysis, and in vitro cellular assays performed on anchorage-dependent and -independent GBM cell lines. This methodological process highlights the potential of repurposable dr

SUBMITTER: Costantini S 

PROVIDER: S-EPMC12683798 | biostudies-literature | 2025 Dec

REPOSITORIES: biostudies-literature