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The Development of HIV-1 Integrase Allosteric Inhibitors Using a Fragment Based Drug Discovery Approach

thesis
posted on 15.07.2018, 09:07 by DAN ZHENG
HIV-1 integrase (IN) is an enzyme that is essential for viral replication. Previous work within our group identified a molecule as a hit that bound to IN and had potential to be developed as an inhibitor of HIV. This thesis describes the hit-to-lead optimisation process of developing the hit into a high-affinity lead compound using a Fragment-Based Drug Discovery approach. Overall, in this work 99 analogues were synthesised and evaluated using multiple assays. The binding affinity of the hit was improved by a factor of 700 thousand.

History

Campus location

Australia

Principal supervisor

David Chalmers

Additional supervisor 1

Martin Scanlon

Additional supervisor 2

Jamie Simpson

Year of Award

2018

Department, School or Centre

Medicinal Chemistry

Additional Institution or Organisation

MIPS

Course

Doctor of Philosophy

Degree Type

DOCTORATE

Faculty

Faculty of Pharmacy and Pharmaceutical Sciences