Design and Synthesis of Styrenylcyclopropylamine LSD1 Inhibitors

[Image: see text] Leveraging the catalytic machinery of LSD1 (KDM1A), a series of covalent styrenylcyclopropane LSD1 inhibitors were identified. These inhibitors represent a new class of mechanism-based inhibitors that target and covalently label the FAD cofactor of LSD1. The series was rapidly prog...

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Bibliografske podrobnosti
izdano v:ACS Med Chem Lett
Main Authors: Gehling, Victor S., McGrath, John P., Duplessis, Martin, Khanna, Avinash, Brucelle, Francois, Vaswani, Rishi G., Côté, Alexandre, Stuckey, Jacob, Watson, Venita, Cummings, Richard T., Balasubramanian, Srividya, Iyer, Priyadarshini, Sawant, Priyanka, Good, Andrew C., Albrecht, Brian K., Harmange, Jean-Christophe, Audia, James E., Bellon, Steven F., Trojer, Patrick, Levell, Julian R.
Format: Artigo
Jezik:Inglês
Izdano: American Chemical Society 2020
Online dostop:https://ncbi.nlm.nih.gov/pmc/articles/PMC7294731/
https://ncbi.nlm.nih.gov/pubmed/32551003
https://ncbi.nlm.nih.govhttp://dx.doi.org/10.1021/acsmedchemlett.0c00060
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