Katherine Creighton

• Master of Pharmacy with Honours
• The synthesis of novel allosteric HIV-1 RT inhibitors

HIV is currently treated using a strategy that involves a combination of medications termed highly active antiretroviral therapy. However, drug resistance is known for all anti-HIV medications and some combination medication regimes have poor safety profiles so there is a need for further drug development.

The enzyme, reverse transcriptase (RT), is required for viral replication and maintenance of long-term infection. Eukaryotic translation elongation factor 1A (eEF1A) has recently been found to bind to RT ultimately facilitating replication of the virus. From virtual screening of RT-eEF1A, several small molecule leads have been found which may hinder replication. The research aim was to use the small molecules discovered to synthesise, characterise and evaluate the various properties of lead compounds for the potential development of drugs against HIV. A novel synthetic route was developed to synthesise lead compounds. The lead compounds were extracted and purified and are to be sent for biological testing.

Funding source: Newcastle University

Project supervisor: Dr Mark Ashton