Article

Pyrimethamine and a potent analogue WCDD115 inhibit NRF2 by suppressing DHFR and one-carbon metabolism

2025-02-17

Abstract excerpt

Nuclear factor erythroid 2-related factor 2 (NFE2L2/NRF2) is a critical mediator of the cellular oxidative stress response. Aberrant activation of NRF2 is common in lung and upper aerodigestive cancers, where it promotes tumor initiation and progression and confers resistance to chemotherapy, radiation therapy, and immune checkpoint inhibitors. As such, NRF2 therapeutic inhibitors are actively being sought. We pre...

Topics

Open a Topic to create a Post that cites this publication.

Identifiers and source

Literature Corpus work: 881ece21-94ef-53b0-8a57-7e275fb2af75
DOI: 10.1101/2025.02.13.637433

Open publication

Related research

Semantic proximity does not establish scientific evidence.

Click a neighbor to travelStep 1 · 12 closest

Pyrimethamine and a potent analogue WCDD115 inhibit NRF2 by suppressing DHFR and one-carbon metabolismDOI 10.1101/2025.02.13.637433Read

Small Molecule Screen Identifies Pyrimethamine as an Inhibitor of NRF2-driven Esophageal HyperplasiaSemantic proximity Read

A Review of Small-Molecule Inhibitors of One-Carbon Enzymes: SHMT2 and MTHFD2 in the SpotlightSemantic proximity Read

A core NRF2 gene set defined through comprehensive transcriptomic analysis predicts selective drug resistance and poor multi-cancer prognosisSemantic proximity Read

More Than a Metabolic Enzyme: MTHFD2 as a Novel Target for Anticancer Therapy?Semantic proximity Read

Nuclear Factor Erythroid 2-Related Factor 2 in Regulating Cancer Metabolism.Semantic proximity Read

Inhibition Of One-Carbon Metabolism In Ewing Sarcoma Results In Profound And Prolonged Growth Suppression Associated With Purine DepletionSemantic proximity Read

Metabolic Reprogramming by Histone Deacetylase Inhibition Selectively Targets NRF2-activated tumorsSemantic proximity Read

A Novel Nrf2 Pathway Inhibitor Sensitizes Keap1-Mutant Lung Cancer Cells to Chemotherapy.Semantic proximity Read

Can't KEEP Up: UXS1 Dependency Exposes a Pyrimidine Vulnerability in KEAP1-Mutant Lung Cancer.Semantic proximity Read

Suppression of NRF2-dependent cancer growth by a covalent allosteric molecular glueSemantic proximity Read

Targeting MTHFD2 disrupts mitochondrial redox homeostasis and restores venetoclax sensitivity in acute myeloid leukemiaSemantic proximity Read

Upregulation of Thymidylate Synthase Induces Pemetrexed Resistance in Malignant Pleural MesotheliomaSemantic proximity Read