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4‐Acyl Pyrroles: Mimicking Acetylated Lysines in Histone Code Reading
Author(s) -
Lucas Xavier,
Wohlwend Daniel,
Hügle Martin,
Schmidtkunz Karin,
Gerhardt Stefan,
Schüle Roland,
Jung Manfred,
Einsle Oliver,
Günther Stefan
Publication year - 2013
Publication title -
angewandte chemie international edition
Language(s) - English
Resource type - Journals
SCImago Journal Rank - 5.831
H-Index - 550
eISSN - 1521-3773
pISSN - 1433-7851
DOI - 10.1002/anie.201307652
Subject(s) - bromodomain , acetylation , histone , reading (process) , epigenetics , chemistry , computational biology , pyrrole , biochemistry , computer science , biology , philosophy , linguistics , dna , gene , organic chemistry
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.