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

doi:10.1002/anie.201307652

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)

Biological Chemistry and Drug Discovery

Research output: Contribution to journal › Article › peer-review

97 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 language	English
Pages (from-to)	14055-14059
Number of pages	5
Journal	Angewandte Chemie International Edition
Volume	52
Issue number	52
Early online date	24 Nov 2013
DOIs	https://doi.org/10.1002/anie.201307652
Publication status	Published - 23 Dec 2013

Keywords

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

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10.1002/anie.201307652

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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.",

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T2 - mimicking acetylated lysines in histone code reading

AU - Lucas, Xavier

AU - Wohlwend, Daniel

AU - Hügle, Martin

AU - Schmidtkunz, Karin

AU - Gerhardt, Stefan

AU - Schüle, Roland

AU - Jung, Manfred

AU - Einsle, Oliver

AU - Günther, Stefan

PY - 2013/12/23

Y1 - 2013/12/23

N2 - 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.

AB - 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.

KW - Acetylation

KW - Histone code

KW - Histones

KW - Humans

KW - Lysine

KW - Pyrroles

KW - Journal article

KW - Research support, Non-U.S. Gov't

U2 - 10.1002/anie.201307652

DO - 10.1002/anie.201307652

M3 - Article

C2 - 24272870

SN - 1433-7851

VL - 52

SP - 14055

EP - 14059

JO - Angewandte Chemie International Edition

JF - Angewandte Chemie International Edition

IS - 52

ER -

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

Abstract

Keywords

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