4-Acyl pyrroles: mimicking acetylated lysines in histone code reading

Xavier Lucas, Daniel Wohlwend, Martin Hügle, Karin Schmidtkunz, Stefan Gerhardt, Roland Schüle, Manfred Jung, Oliver Einsle, Stefan Günther (Lead / Corresponding author)

Research output: Contribution to journalArticle

73 Citations (Scopus)

Abstract

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.
Original languageEnglish
Pages (from-to)14055-14059
Number of pages5
JournalAngewandte Chemie International Edition
Volume52
Issue number52
Early online date24 Nov 2013
DOIs
Publication statusPublished - 23 Dec 2013

Keywords

  • Acetylation
  • Histone code
  • Histones
  • Humans
  • Lysine
  • Pyrroles
  • Journal article
  • Research support, Non-U.S. Gov't

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    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