Fragment-Based Screening of the Bromodomain of ATAD2
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 crysta...
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| Veröffentlicht in: | Journal of medicinal chemistry 2014-11, Vol.57 (22), p.9687-9692 |
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| container_end_page | 9692 |
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| container_issue | 22 |
| container_start_page | 9687 |
| container_title | Journal of medicinal chemistry |
| container_volume | 57 |
| creator | Harner, Mary J Chauder, Brian A Phan, Jason Fesik, Stephen W |
| description | 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. |
| doi_str_mv | 10.1021/jm501035j |
| format | Article |
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| identifier | ISSN: 0022-2623 |
| ispartof | Journal of medicinal chemistry, 2014-11, Vol.57 (22), p.9687-9692 |
| issn | 0022-2623 1520-4804 |
| language | eng |
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| source | MEDLINE; American Chemical Society Journals |
| subjects | 60 APPLIED LIFE SCIENCES Adenosine Triphosphatases - chemistry Antineoplastic Agents - chemistry ATPases Associated with Diverse Cellular Activities BASIC BIOLOGICAL SCIENCES Binding Sites Brief Chemistry, Pharmaceutical - methods Crystallography, X-Ray - methods DNA-Binding Proteins - chemistry Humans Kinetics Ligands Magnetic Resonance Spectroscopy - methods Molecular Conformation Neoplasms - drug therapy Protein Structure, Tertiary |
| title | Fragment-Based Screening of the Bromodomain of ATAD2 |
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