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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...
Autores principales: | , , , |
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Formato: | Online Artículo Texto |
Lenguaje: | English |
Publicado: |
American Chemical
Society
2014
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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. |
format | Online Article Text |
id | pubmed-4255743 |
institution | National Center for Biotechnology Information |
language | English |
publishDate | 2014 |
publisher | American Chemical
Society |
record_format | MEDLINE/PubMed |
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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