Please use this identifier to cite or link to this item: doi:10.22028/D291-30928
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Title: Rational Adaptation of L3MBTL1 Inhibitors to Create Small-Molecule Cbx7 Antagonists
Author(s): Simhadri, Chakravarthi
Daze, Kevin D.
Douglas, Sarah F.
Milosevich, Natalia
Monjas, Leticia
Dev, Amarjot
Brown, Tyler M.
Hirsch, Anna
Wulff, Jeremy E.
Hof, Fraser
Language: English
Title: ChemMedChem : chemistry enabling drug discovery
Volume: 14
Issue: 15
Startpage: 1444
Endpage: 1456
Publisher/Platform: Wiley-VCH
Year of Publication: 2019
Publikation type: Journal Article
Abstract: Chromobox homolog 7 (Cbx7) is an epigenetic modulator that is an important driver of multiple cancers. It is a methyl reader protein that operates by recognizing and binding to methylated lysine residues on specific partners. Herein we report our efforts to create low-molecular-weight inhibitors of Cbx7 by making rational structural adaptations to inhibitors of a different methyl reader protein, L3MBTL1, inhibitors that had previously been reported to be inactive against Cbx7. We evaluated each new inhibitor for Cbx7 inhibition by fluorescence polarization assay, and also confirmed the binding of selected inhibitors to Cbx7 by saturation-transfer difference NMR spectroscopy. This work identified multiple small-molecule inhibitors with modest (IC50 : 257-500 μm) potency.
DOI of the first publication: 10.1002/cmdc.201900021
URL of the first publication: https://chemistry-europe.onlinelibrary.wiley.com/doi/full/10.1002/cmdc.201900021
Link to this record: hdl:20.500.11880/29143
http://dx.doi.org/10.22028/D291-30928
ISSN: 1860-7187
1860-7179
Date of registration: 14-May-2020
Faculty: NT - Naturwissenschaftlich- Technische Fakultät
Department: NT - Pharmazie
Professorship: NT - Prof. Dr. Anna Hirsch
Collections:UniBib – Die Universitätsbibliographie

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