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