| Autor: |
Venita G. Watson, Richard T. Cummings, Victor S. Gehling, Andrew C. Good, Brian K. Albrecht, Priyanka Sawant, John P. McGrath, James E. Audia, Jean-Christophe Harmange, Priyadarshini Iyer, Rishi G. Vaswani, Srividya Balasubramanian, Alexandre Côté, Avinash Khanna, Steven Bellon, Francois Brucelle, Julian Levell, Patrick Trojer, Jacob I. Stuckey, Martin Duplessis |
| Rok vydání: |
2020 |
| Předmět: |
|
| Zdroj: |
ACS Med Chem Lett |
| ISSN: |
1948-5875 |
| Popis: |
[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 progressed to potent biochemical and cellular LSD1 inhibitors with good physical properties. This effort resulted in the identification of 34, a highly potent ( |
| Databáze: |
OpenAIRE |
| Externí odkaz: |
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