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Borrello, Maria Teresa, Schinor, Benjamin, Bartels, Katharina, Benelkebir, Hanae, Pereira, Sara, Al-Jamal, Wafa T., Douglas, Leon, Duriez, Patrick J., Packham, Graham, Haufe, Günter and Ganesan, A. 
ORCID: https://orcid.org/0000-0003-4862-7999
(2017)
Fluorinated tranylcypromine analogues as inhibitors of lysine-specific demethylase 1 (LSD1, KDM1A).
Bioorganic & Medicinal Chemistry Letters, 27 (10).
2099–2101.
ISSN 0960-894X
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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.
| Item Type: | Article |
|---|---|
| Uncontrolled Keywords: | organofluorine compounds,epigenetics,fad-dependent enzymes,lysine demethylase,mechanism based inhibitors |
| Faculty \ School: | Faculty of Science Faculty of Science > School of Pharmacy (former - to 2024) |
| UEA Research Groups: | Faculty of Science > Research Groups > Drug Delivery and Pharmaceutical Materials (former - to 2017) Faculty of Science > Research Groups > Medicinal Chemistry (former - to 2017) Faculty of Science > Research Groups > Chemical Biology and Medicinal Chemistry (former - to 2021) |
| Related URLs: | |
| Depositing User: | Pure Connector |
| Date Deposited: | 06 Apr 2017 06:59 |
| Last Modified: | 21 Dec 2024 00:52 |
| URI: | https://ueaeprints.uea.ac.uk/id/eprint/63177 |
| DOI: | 10.1016/j.bmcl.2017.03.081 |
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