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Fragment-Based Screening of the Bromodomain of ATAD2

[Image: see text] Cellular and genetic evidence suggest that inhibition of ATAD2 could be a useful strategy to treat several types of cancer. To discover small-molecule inhibitors of the bromodomain of ATAD2, we used a fragment-based approach. Fragment hits were identified using NMR spectroscopy, an...

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Autores principales: Harner, Mary J., Chauder, Brian A., Phan, Jason, Fesik, Stephen W.
Formato: Online Artículo Texto
Lenguaje:English
Publicado: American Chemical Society 2014
Acceso en línea:https://www.ncbi.nlm.nih.gov/pmc/articles/PMC4255743/
https://www.ncbi.nlm.nih.gov/pubmed/25314628
http://dx.doi.org/10.1021/jm501035j
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author Harner, Mary J.
Chauder, Brian A.
Phan, Jason
Fesik, Stephen W.
author_facet Harner, Mary J.
Chauder, Brian A.
Phan, Jason
Fesik, Stephen W.
author_sort Harner, Mary J.
collection PubMed
description [Image: see text] Cellular and genetic evidence suggest that inhibition of ATAD2 could be a useful strategy to treat several types of cancer. To discover small-molecule inhibitors of the bromodomain of ATAD2, we used a fragment-based approach. Fragment hits were identified using NMR spectroscopy, and ATAD2 was crystallized with three of the hits identified in the fragment screen.
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spelling pubmed-42557432015-10-14 Fragment-Based Screening of the Bromodomain of ATAD2 Harner, Mary J. Chauder, Brian A. Phan, Jason Fesik, Stephen W. J Med Chem [Image: see text] Cellular and genetic evidence suggest that inhibition of ATAD2 could be a useful strategy to treat several types of cancer. To discover small-molecule inhibitors of the bromodomain of ATAD2, we used a fragment-based approach. Fragment hits were identified using NMR spectroscopy, and ATAD2 was crystallized with three of the hits identified in the fragment screen. American Chemical Society 2014-10-14 2014-11-26 /pmc/articles/PMC4255743/ /pubmed/25314628 http://dx.doi.org/10.1021/jm501035j Text en Copyright © 2014 American Chemical Society This is an open access article published under an ACS AuthorChoice License (http://pubs.acs.org/page/policy/authorchoice_termsofuse.html) , which permits copying and redistribution of the article or any adaptations for non-commercial purposes.
spellingShingle Harner, Mary J.
Chauder, Brian A.
Phan, Jason
Fesik, Stephen W.
Fragment-Based Screening of the Bromodomain of ATAD2
title Fragment-Based Screening of the Bromodomain of ATAD2
title_full Fragment-Based Screening of the Bromodomain of ATAD2
title_fullStr Fragment-Based Screening of the Bromodomain of ATAD2
title_full_unstemmed Fragment-Based Screening of the Bromodomain of ATAD2
title_short Fragment-Based Screening of the Bromodomain of ATAD2
title_sort fragment-based screening of the bromodomain of atad2
url https://www.ncbi.nlm.nih.gov/pmc/articles/PMC4255743/
https://www.ncbi.nlm.nih.gov/pubmed/25314628
http://dx.doi.org/10.1021/jm501035j
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