Development of Potent AspH Inhibitors as Novel Small-Molecule Anti-Cancer Therapeutics

University of Oxford

Thomas is investigating how the inhibition of a specific human enzyme could be developed into a potential cancer therapy. The enzyme AspH appears more frequently in several human cancer cells, including pancreatic, bile duct and liver cancer. There is clear link between this enzyme and increased mortality rates from these cancers, so Thomas is investigating how stopping this enzyme could be an effective novel cancer treatment. The goal of his research is to design and synthesise an enzyme inhibitor to prevent the action of AspH, and then to evaluate its effectiveness in treating cancer.

Current inhibitors of the AspH enzyme have suffered from a lack of research. Many exhibit limited selectivity or ability to enter cells. Thomas’s project will exploit this gap in the pharmacological market, for the benefit of millions of patients worldwide. Ineffective medicines of this type can cause dangerous side-effects in other regions of the body. The research into this area will also have relevance for the treatment of other diseases affected by related human enzymes, including anaemia and inflammation.

Thomas is a graduate from the University of Cambridge, where he studied Natural Sciences. For his master’s project he researched the application of “click” technology in the synthesis of supramolecular architecture, and for this work he was awarded the Emeleus Prize for Inorganic Chemistry. Thomas has previously completed a 10-week internship at AstraZeneca. He is currently a PhD student in the Synthesis for Biology and Medicine CDT at the University of Oxford, working in collaboration with GlaxoSmithKline.

"We envisage that this work will be extremely valuable towards the development of new treatments for pancreatic cancer, hepatocellular carcinoma, and bile duct cancer. Furthermore, if successful, this drug discovery approach could be applicable to many other closely related human enzymes, several of which are currently being investigated as therapeutic targets for anaemia, inflammation, and cancer."