Chemical epigenetics: the impact of chemical and chemical biology techniques on bromodomain target validation

Epigenetics is currently the focus of intense research interest across a broad range of disciplines due to its importance in a multitude of biological processes and disease states. Epigenetic functions result partly from modification of the nucleobases in DNA and RNA, and/or post‐translational modif...

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Main Authors: Schiedel, M, Moroglu, M, Ascough, D, Chamberlain, A, Kamps, J, Sekirnik, A, Conway, S
Format: Journal article
Language:English
Published: Wiley 2019
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author Schiedel, M
Moroglu, M
Ascough, D
Chamberlain, A
Kamps, J
Sekirnik, A
Conway, S
author_facet Schiedel, M
Moroglu, M
Ascough, D
Chamberlain, A
Kamps, J
Sekirnik, A
Conway, S
author_sort Schiedel, M
collection OXFORD
description Epigenetics is currently the focus of intense research interest across a broad range of disciplines due to its importance in a multitude of biological processes and disease states. Epigenetic functions result partly from modification of the nucleobases in DNA and RNA, and/or post‐translational modifications of histone proteins. These modifications are dynamic, with cellular machinery identified to modulate and interpret the marks. Our focus is on bromodomains, which bind to acetylated lysine residues. Progress in the study of bromodomains, and the development of bromodomain ligands, has been rapid. These advances have been underpinned by many disciplines, but chemistry and chemical biology have undoubtedly played a significant role. Herein, we review the key chemistry and chemical biology approaches that have furthered our study of bromodomains, enabled the development of bromodomain ligands, and played a critical role in the validation of bromodomains as therapeutic targets.
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spelling oxford-uuid:546d8049-e2d9-4ad9-b76e-f474de3f75932022-03-26T16:37:47ZChemical epigenetics: the impact of chemical and chemical biology techniques on bromodomain target validationJournal articlehttp://purl.org/coar/resource_type/c_dcae04bcuuid:546d8049-e2d9-4ad9-b76e-f474de3f7593EnglishSymplectic Elements at OxfordWiley2019Schiedel, MMoroglu, MAscough, DChamberlain, AKamps, JSekirnik, AConway, SEpigenetics is currently the focus of intense research interest across a broad range of disciplines due to its importance in a multitude of biological processes and disease states. Epigenetic functions result partly from modification of the nucleobases in DNA and RNA, and/or post‐translational modifications of histone proteins. These modifications are dynamic, with cellular machinery identified to modulate and interpret the marks. Our focus is on bromodomains, which bind to acetylated lysine residues. Progress in the study of bromodomains, and the development of bromodomain ligands, has been rapid. These advances have been underpinned by many disciplines, but chemistry and chemical biology have undoubtedly played a significant role. Herein, we review the key chemistry and chemical biology approaches that have furthered our study of bromodomains, enabled the development of bromodomain ligands, and played a critical role in the validation of bromodomains as therapeutic targets.
spellingShingle Schiedel, M
Moroglu, M
Ascough, D
Chamberlain, A
Kamps, J
Sekirnik, A
Conway, S
Chemical epigenetics: the impact of chemical and chemical biology techniques on bromodomain target validation
title Chemical epigenetics: the impact of chemical and chemical biology techniques on bromodomain target validation
title_full Chemical epigenetics: the impact of chemical and chemical biology techniques on bromodomain target validation
title_fullStr Chemical epigenetics: the impact of chemical and chemical biology techniques on bromodomain target validation
title_full_unstemmed Chemical epigenetics: the impact of chemical and chemical biology techniques on bromodomain target validation
title_short Chemical epigenetics: the impact of chemical and chemical biology techniques on bromodomain target validation
title_sort chemical epigenetics the impact of chemical and chemical biology techniques on bromodomain target validation
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AT moroglum chemicalepigeneticstheimpactofchemicalandchemicalbiologytechniquesonbromodomaintargetvalidation
AT ascoughd chemicalepigeneticstheimpactofchemicalandchemicalbiologytechniquesonbromodomaintargetvalidation
AT chamberlaina chemicalepigeneticstheimpactofchemicalandchemicalbiologytechniquesonbromodomaintargetvalidation
AT kampsj chemicalepigeneticstheimpactofchemicalandchemicalbiologytechniquesonbromodomaintargetvalidation
AT sekirnika chemicalepigeneticstheimpactofchemicalandchemicalbiologytechniquesonbromodomaintargetvalidation
AT conways chemicalepigeneticstheimpactofchemicalandchemicalbiologytechniquesonbromodomaintargetvalidation