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Structure-based approaches towards identification of fragments for the low-druggability ATAD2 bromodomain

Abstract:

The transcriptional co-regulator ATAD2 is a prognostic marker for patient survival in many cancers. ATAD2 harbours a bromodomain which may offer an opportunity for pharmacological intervention, but its shallow, polar binding surface makes the development of inhibitors challenging. Here we optimized crystal transfer/soaking conditions enabling crystallographic fragment screening. We describe nine crystal structures of fragments including thymidine, a novel acetyl-lysine mimetic ligand and the ...

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Publication status:
Published

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Publisher copy:
10.1039/c4md00237g

Authors


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Institution:
University of Oxford
Department:
Oxford, MSD, Clinical Medicine, Structural Genomics Consortium
Role:
Author
Publisher:
Royal Society of Chemistry
Journal:
MEDCHEMCOMM
Volume:
5
Issue:
12
Pages:
1843-1848
Publication date:
2014-01-01
DOI:
EISSN:
2040-2511
ISSN:
2040-2503
URN:
uuid:9dd41f9b-0290-446d-a506-1595a4210bb7
Source identifiers:
492475
Local pid:
pubs:492475
Language:
English

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