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Epigenetic Drug Discovery: Bromodomain Inhibitors

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posted on 26.03.2019 by JOSEPH PHILLIP HILTON-PROCTOR
Bromodomains are one of many proteins tasked with regulating certain genes. They have been of great interest as drug targets due to their connection to diseases such as cancer. Despite the significant amount of work that has gone into developing inhibitors that prevent their binding activity, two compounds have yet to be explored as potential inhibitors. Using three different approaches to Fragment-based Drug Design, we have elaborated on N-Methylpyrrolidone and 5-methyl-3-aryl-1H-pyrazole as potential bromodomain inhibitor candidates. This work has resulted in the development of several lead compounds with improved inhibition and crystal structures that have helped rationalise their activity.

History

Campus location

Australia

Principal supervisor

Philip Thompson

Additional supervisor 1

Martin Scanlon

Year of Award

2019

Department, School or Centre

Medicinal Chemistry

Additional Institution or Organisation

Monash Institute of Pharmaceutical Sciences

Course

Doctor of Philosophy

Degree Type

DOCTORATE

Faculty

Faculty of Pharmacy and Pharmaceutical Sciences

Exports