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Journal articles
Novel 3,5-bis(bromohydroxybenzylidene)piperidin-4-ones as coactivator-associated arginine methyltransferase 1 inhibitors: enzyme selectivity and cellular activity.
Abstract : Coactivator-associated arginine methyltransferase 1 (CARM1) represents a valuable target for hormone-dependent tumors such as prostate and breast cancers. Here we report the enzyme and cellular characterization of the 1-benzyl-3,5-bis(3-bromo-4-hydroxybenzylidene)piperidin-4-one (7g) and its analogues 8a-l. Among them, 7g, 8e, and 8l displayed high and selective CARM1 inhibition, with lower or no activity against a panel of different PRMTs or HKMTs. In human LNCaP cells, 7g showed a significant dose-dependent reduction of the PSA promoter activity.
Cited literature [24 references]
https://hal-riip.archives-ouvertes.fr/pasteur-00968654
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Submitted on : Tuesday, April 1, 2014 - 12:48:45 PM
Last modification on : Wednesday, November 3, 2021 - 2:18:08 PM
Long-term archiving on: : Monday, April 10, 2017 - 8:16:11 AM
Contributor : Istituto Pasteur Fondazione Cenci Bolognetti Connect in order to contact the contributor
Submitted on : Tuesday, April 1, 2014 - 12:48:45 PM
Last modification on : Wednesday, November 3, 2021 - 2:18:08 PM
Long-term archiving on: : Monday, April 10, 2017 - 8:16:11 AM
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Chengetal2011.pdf
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