| LECOINTRE, Bertrand, Remy NAROZNY, Maria Teresa BORRELLO, Johanna SENGER, Alokta CHAKRABARTI, Manfred JUNG, Martin MAREK, Christophe ROMIER, Jelena MELESINA, Wolfgang SIPPL, Laurent BISCHOFF a A. GANESAN. Isoform-selective HDAC1/16/8 inhibitors with an imidazo-ketopiperazine cap containing stereochemical diversity. PHILOSOPHICAL TRANSACTIONS OF THE ROYAL SOCIETY B-BIOLOGICAL SCIENCES. LONDON: ROYAL SOC, 2018, roč. 373, č. 1748, s. 1-7. ISSN 0962-8436. Dostupné z: https://dx.doi.org/10.1098/rstb.2017.0364. |
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@article{1495537,
author = {Lecointre, Bertrand and Narozny, Remy and Borrello, Maria Teresa and Senger, Johanna and Chakrabarti, Alokta and Jung, Manfred and Marek, Martin and Romier, Christophe and Melesina, Jelena and Sippl, Wolfgang and Bischoff, Laurent and Ganesan, A.},
article_location = {LONDON},
article_number = {1748},
doi = {http://dx.doi.org/10.1098/rstb.2017.0364},
keywords = {zinc metalloenzymes; epigenetics; histone deacetylases; enzyme inhibitors; peptidomimetics},
language = {eng},
issn = {0962-8436},
journal = {PHILOSOPHICAL TRANSACTIONS OF THE ROYAL SOCIETY B-BIOLOGICAL SCIENCES},
title = {Isoform-selective HDAC1/16/8 inhibitors with an imidazo-ketopiperazine cap containing stereochemical diversity},
url = {https://royalsocietypublishing.org/doi/10.1098/rstb.2017.0364},
volume = {373},
year = {2018}
}
TY - JOUR
ID - 1495537
AU - Lecointre, Bertrand - Narozny, Remy - Borrello, Maria Teresa - Senger, Johanna - Chakrabarti, Alokta - Jung, Manfred - Marek, Martin - Romier, Christophe - Melesina, Jelena - Sippl, Wolfgang - Bischoff, Laurent - Ganesan, A.
PY - 2018
TI - Isoform-selective HDAC1/16/8 inhibitors with an imidazo-ketopiperazine cap containing stereochemical diversity
JF - PHILOSOPHICAL TRANSACTIONS OF THE ROYAL SOCIETY B-BIOLOGICAL SCIENCES
VL - 373
IS - 1748
SP - 1-7
EP - 1-7
PB - ROYAL SOC
SN - 09628436
KW - zinc metalloenzymes
KW - epigenetics
KW - histone deacetylases
KW - enzyme inhibitors
KW - peptidomimetics
UR - https://royalsocietypublishing.org/doi/10.1098/rstb.2017.0364
L2 - https://royalsocietypublishing.org/doi/10.1098/rstb.2017.0364
N2 - A series of hvdroxamic acids linked by different lengths to a chiral imidazo-ketopiperazine scaffold were synthesized. The compounds with linker lengths of 6 and 7 ca vb on atoms were the most potent in histone deacetylase (HDAC) inhibition, and were specific submicromolar inhibitors of the HDAC1, HDAC6 and HDAC8 isoforms. A docking model for the binding mode predicts binding of the hvdroxamic acid to the active site zinc cation and additional interactions between the imidazo-ketopiperazine and the enzyme rim. The compounds were micromolar inhibitors of the MV4-11, THP-1 and U937 cancer cell lines. Increased levels of histone H3 and tubulin acetylation support a cellular mechanism of action through HDAC inhibition. This article is part of a discussion meeting issue 'Frontiers in epigenetic chemical biology'.
ER -
LECOINTRE, Bertrand, Remy NAROZNY, Maria Teresa BORRELLO, Johanna SENGER, Alokta CHAKRABARTI, Manfred JUNG, Martin MAREK, Christophe ROMIER, Jelena MELESINA, Wolfgang SIPPL, Laurent BISCHOFF a A. GANESAN. Isoform-selective HDAC1/16/8 inhibitors with an imidazo-ketopiperazine cap containing stereochemical diversity. \textit{PHILOSOPHICAL TRANSACTIONS OF THE ROYAL SOCIETY B-BIOLOGICAL SCIENCES}. LONDON: ROYAL SOC, 2018, roč.~373, č.~1748, s.~1-7. ISSN~0962-8436. Dostupné z: https://dx.doi.org/10.1098/rstb.2017.0364.
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