Thesis
Development of small molecule inhibitors of the bromodomain-histone interaction
- Abstract:
-
Bromodomains bind to acetylated lysine residues 1 to mediate a wide range of biological processes, including the assembly of transcriptional machinery at modified histones. This thesis describes the design of small molecule inhibitors of bromodomains, with particular focus on the bromodomain of CREBBP.
A fragment based approach was employed to investigate bicyclic amides as acetyl lysine mimics. Initially the benzoxazinone scaffold (BNZ) 2 was shown to be a novel, ligand efficient b...
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Authors
Contributors
+ Stuart J Conway
Role:
Supervisor
+ Paul E Brennan
Role:
Supervisor
+ Timothy Patrick Christopher Rooney
Institution:
University of Oxford
Research group:
Prof Stuart Conway
Oxford college:
St Catherine's College
Department:
Mathematical,Physical & Life Sciences Division - Chemistry - Organic Chemistry
Funding
+ Oxford University Doctoral Training Centres; Engineering and Physical Sciences Research Council; Pfizer
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Funding agency for:
Timothy Patrick Christopher Rooney
Bibliographic Details
- Publication date:
- 2014
- Type of award:
- DPhil
- Level of award:
- Doctoral
- URN:
-
uuid:dfe22076-befc-4881-8433-b563a9329478
- Local pid:
- ora:12217
Item Description
- Language:
- English
- Keywords:
- Subjects:
Terms of use
- Copyright holder:
- Timothy P C Rooney
- Copyright date:
- 2014
- Notes:
- This thesis is not currently available via ORA.
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