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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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Role:
Supervisor
Role:
Supervisor
Institution:
University of Oxford
Research group:
Prof Stuart Conway
Oxford college:
St Catherine's College
Department:
Mathematical,Physical & Life Sciences Division - Chemistry - Organic Chemistry
Publication date:
2014
Type of award:
DPhil
Level of award:
Doctoral
URN:
uuid:dfe22076-befc-4881-8433-b563a9329478
Local pid:
ora:12217

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