Bromodomains are acetyllysine epigenetic mark reader proteins. Small molecules inhibiting them have potential as anti-inflammatory, antiviral, and anticancer agents. A 4-acyl pyrrole derivative (see yellow structure in recognition pocket) has been identified that potently inhibits specific bromodomains and exhibits antiproliferative activity against leukemia cell lines.
- Histone code
- Journal article
- Research support, Non-U.S. Gov't
Lucas, X., Wohlwend, D., Hügle, M., Schmidtkunz, K., Gerhardt, S., Schüle, R., Jung, M., Einsle, O., & Günther, S. (2013). 4-Acyl pyrroles: mimicking acetylated lysines in histone code reading. Angewandte Chemie International Edition, 52(52), 14055-14059. https://doi.org/10.1002/anie.201307652