Bromodomain protein inhibition: a novel therapeutic strategy in rheumatic diseases

The reading of acetylation marks on histones by bromodomain (BRD) proteins is a key event in transcriptional activation. Small molecule inhibitors targeting bromodomain and extra-terminal (BET) proteins compete for binding to acetylated histones. They have strong anti-inflammatory properties and exh...

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Detalles Bibliográficos
Autor principal: Klein, Kerstin
Formato: Online Artículo Texto
Lenguaje:English
Publicado: BMJ Publishing Group 2018
Materias:
Animal Models
Acceso en línea:https://www.ncbi.nlm.nih.gov/pmc/articles/PMC6269638/
https://www.ncbi.nlm.nih.gov/pubmed/30564450
http://dx.doi.org/10.1136/rmdopen-2018-000744
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author Klein, Kerstin
author_facet Klein, Kerstin
author_sort Klein, Kerstin
collection PubMed
description The reading of acetylation marks on histones by bromodomain (BRD) proteins is a key event in transcriptional activation. Small molecule inhibitors targeting bromodomain and extra-terminal (BET) proteins compete for binding to acetylated histones. They have strong anti-inflammatory properties and exhibit encouraging effects in different cell types in vitro and in animal models resembling rheumatic diseases in vivo. Furthermore, recent studies that focus on BRD proteins beyond BET family members are discussed.
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spelling pubmed-62696382018-12-18 Bromodomain protein inhibition: a novel therapeutic strategy in rheumatic diseases Klein, Kerstin RMD Open Animal Models The reading of acetylation marks on histones by bromodomain (BRD) proteins is a key event in transcriptional activation. Small molecule inhibitors targeting bromodomain and extra-terminal (BET) proteins compete for binding to acetylated histones. They have strong anti-inflammatory properties and exhibit encouraging effects in different cell types in vitro and in animal models resembling rheumatic diseases in vivo. Furthermore, recent studies that focus on BRD proteins beyond BET family members are discussed. BMJ Publishing Group 2018-11-16 /pmc/articles/PMC6269638/ /pubmed/30564450 http://dx.doi.org/10.1136/rmdopen-2018-000744 Text en © Author(s) (or their employer(s)) 2018. Re-use permitted under CC BY-NC. No commercial re-use. See rights and permissions. Published by BMJ. This is an open access article distributed in accordance with the Creative Commons Attribution Non Commercial (CC BY-NC 4.0) license, which permits others to distribute, remix, adapt, build upon this work non-commercially, and license their derivative works on different terms, provided the original work is properly cited, appropriate credit is given, any changes made indicated, and the use is non-commercial. See: http://creativecommons.org/licenses/by-nc/4.0
spellingShingle Animal Models
Klein, Kerstin
Bromodomain protein inhibition: a novel therapeutic strategy in rheumatic diseases
title Bromodomain protein inhibition: a novel therapeutic strategy in rheumatic diseases
title_full Bromodomain protein inhibition: a novel therapeutic strategy in rheumatic diseases
title_fullStr Bromodomain protein inhibition: a novel therapeutic strategy in rheumatic diseases
title_full_unstemmed Bromodomain protein inhibition: a novel therapeutic strategy in rheumatic diseases
title_short Bromodomain protein inhibition: a novel therapeutic strategy in rheumatic diseases
title_sort bromodomain protein inhibition: a novel therapeutic strategy in rheumatic diseases
topic Animal Models
url https://www.ncbi.nlm.nih.gov/pmc/articles/PMC6269638/
https://www.ncbi.nlm.nih.gov/pubmed/30564450
http://dx.doi.org/10.1136/rmdopen-2018-000744
work_keys_str_mv AT kleinkerstin bromodomainproteininhibitionanoveltherapeuticstrategyinrheumaticdiseases

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