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Excel · study · 2026

Small molecule MYC Inhibitor restricts ovarian tumor growth by suppressing c-Myc mediated glycolysis

Listed in NCBI GEO

Ovarian cancer is characterized by aberrant cMYC expression and dysregulated glycolysis. cMYC overexpression is linked to poorer patient survival.

Description

Since MYC protein is not part of a receptor-ligand pair and lacks a defined binding site for small molecules, MYC inhibitors are not yet available for clinical applications. Herein, we report the discovery of GD-07 a small molecule identified through high-throughput in silico screening that binds with G-quadruplex (G4) motif in c-Myc promoter.

GD-07 effectively stabilizes MYC-G4 through a combination of electrostatic and noncovalent interactions. GD-07 exhibits high cytotoxicity in ovarian cancer cells (A2780) with minimal toxicity in normal cells, providing a wide therapeutic window for targeted cancer therapy. GD-07 suppresses c-Myc expression in ovarian cancer cells, which in turn curtails glucose metabolism and glycolysis.

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This suppression is accompanied by the promotion of p53 and pro-apoptotic markers, indicating a potential induction of cancer cell apoptosis. Notably, GD-07 exhibit superior efficacy to carboplatin in patient-derived organoids of high-grade serous ovarian cancer (HGSOC), effectively mimicking clinical responses. GD-07 disrupts metabolic pathways and induces apoptosis by modulating key oncogenic and tumor suppressor genes.

Our findings highlight GD-07 as a promising therapeutic agent that selectively targets the c-Myc G-quadruplex and disrupts bioenergetics, offering a dual mechanism of action by inhibiting proliferation and promoting apoptosis. GD-07 represents a novel approach with high translational potential for treating resistant and metastatic ovarian cancer, laying the foundation for future development of next-generation cancer therapeutics.

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Life Sciences
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Cancer 75%
Provenance · 1 source records, 8 field assertions
SourceKeyLast seenRaw
NCBI GEOGSE29727413 d agoJSON v1
FieldAssertionExtractorEvidence
access_levelsource · NCBI GEOconnector:ncbi_geo@1.0.0
concepts[disease].local:disease:cancerenrichment · NCBI GEOkeyword-concept-rules@1.0.0title+description (75%)
concepts[field].local:field:life-sciencesmapping · NCBI GEOconnector:ncbi_geo@1.0.0
concepts[method].geo_series_type:expression-profiling-by-high-throughput-sequencingsource · NCBI GEOconnector:ncbi_geo@1.0.0/gdstype
concepts[organism].NCBITaxon:9606source · NCBI GEOconnector:ncbi_geo@1.0.0/taxon
descriptionsource · NCBI GEOconnector:ncbi_geo@1.0.0/summary
publication_datesource · NCBI GEOconnector:ncbi_geo@1.0.0
titlesource · NCBI GEOconnector:ncbi_geo@1.0.0/title