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Literature summary for 1.14.11.67 extracted from

  • Pippa, S.; Mannironi, C.; Licursi, V.; Bombardi, L.; Colotti, G.; Cundari, E.; Mollica, A.; Coluccia, A.; Naccarato, V.; La Regina, G.; Silvestri, R.; Negri, R.
    Small molecule inhibitors of KDM5 histone demethylases increase the radiosensitivity of breast cancer cells overexpressing JARID1B (2019), Molecules, 24, 1739 .
    View publication on PubMedView publication on EuropePMC
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Inhibitors

Inhibitors Comment Organism Structure
ethyl 1-[3-[(4-methoxybenzene-1-sulfonyl)amino]benzoyl]prolinate upon treatment with 30 microM, a strong increase of cells in G2/M and of the subG1 fraction is noted Homo sapiens
ethyl 2-[3-[(4-methoxybenzene-1-sulfonyl)amino]benzoyl]benzoate compound can selectively inhibit KDM5 enzymes and is capable of increasing sensitivity of breast cancer cells to ionizing radiation and radiation-induced damage. The compound does not show any significant effect on cell cycle Homo sapiens
KDOAM-25 inhibits KDM5 enzymes in vitro with IC50 below 100 nM. In MCF-7 cells, it induces an increase of H3K4me3 levels at 0.03-1 microM. The compound does not show any significant effect on cell cycle Homo sapiens

Organism

Organism UniProt Comment Textmining
Homo sapiens Q9UGL1
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Source Tissue

Source Tissue Comment Organism Textmining
MCF-7 cell
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 Homo sapiens
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General Information

General Information Comment Organism
physiological function KDM5B is not a strong transcriptional repressor but rather a fine-tuning regulator of cell type-specific H3K4 methylation and transcript levels. The top up-regulated genes CYP1A1, CYP1B2, ALDH1A3 and AHRR are involved in the aryl hydrocarbon receptor (AhR) response Homo sapiens