Fluorinated tranylcypromine analogues as inhibitors of lysine-specific deme-thylase 1 (LSD1, KDM1A
Borrello, Maria Teresa, Schinor, Benjamin, Bartels, Katharina, Benelkebir, Hanae, Pereira, Sara, Al-Jamal, Wafa T, Douglas, Leon, Duriez, Patrick J, Packham, Graham, Haufe, Gunter and Ganesan, A (2017) Fluorinated tranylcypromine analogues as inhibitors of lysine-specific deme-thylase 1 (LSD1, KDM1A. Bioorganic and Medicinal Chemistry Letters, 27 (10). pp. 2099-2101. ISSN 0960-894X
| Item Type: | Article |
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Abstract
We report a series of tranylcypromine analogues containing a fluorine in the cyclopropyl ring. A number of compounds with additional m- or p- substitution of the aryl ring were micromolar inhibitors of the LSD1 enzyme. In cellular assays, the compounds inhibited the proliferation of acute myeloid leukemia cell lines. Increased levels of the biomarkers H3K4me2 and CD86 were consistent with LSD1 target engagement
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More Information
| Uncontrolled Keywords: Organofluorine compounds Epigenetics FAD-dependent enzymes Lysine demethylase Mechanism based inhibitors |
| Depositing User: Teresa Borrello |
Identifiers
| Item ID: 15995 |
| Identification Number: https://doi.org/10.1016/j.bmcl.2017.03.081 |
| ISSN: 0960-894X |
| URI: http://sure.sunderland.ac.uk/id/eprint/15995 | Official URL: https://doi.org/10.1016/j.bmcl.2017.03.081 |
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Catalogue record
| Date Deposited: 18 Sep 2023 08:54 |
| Last Modified: 18 Sep 2023 08:54 |
| Author: |
Maria Teresa Borrello
|
| Author: | Benjamin Schinor |
| Author: | Katharina Bartels |
| Author: | Hanae Benelkebir |
| Author: | Sara Pereira |
| Author: | Wafa T Al-Jamal |
| Author: | Leon Douglas |
| Author: | Patrick J Duriez |
| Author: | Graham Packham |
| Author: | Gunter Haufe |
| Author: | A Ganesan |
University Divisions
Faculty of Health Sciences and Wellbeing > School of Pharmacy and Pharmaceutical SciencesSubjects
Sciences > ChemistrySciences > Pharmacy and Pharmacology
Sciences
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