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Worldwide cancer research announces that the Curestarters project which enabled  Professor John Spencer Sussex Drug Discovery Centre and others to carry out vital research on p53 has enabled a new cancer treatment called Rezatapopt to enter clinical trials. The p53 gene is mutated more than any other in cancer but it is often referred to as the 'guardian of the genome' because of its vital role in controlling DNA repair and cell division.

Prof Spencer added ‘I am delighted to see that Rezatapopt has now entered clinical trials for patients with advanced solid tumours, and I hope that in the future it will go on to help many more cancer patients. New treatments like this wouldn’t be possible without discovery research so thank you to the Curestarters who helped us make breakthroughs that others have built upon to make their important discoveries’.

Professor Spencer, lead Medicinal Chemist at the Sussex Drug Discovery Centre, teamed up with p53 experts Sir Alan Fersht and Dr Andreas Joerger in Cambridge (now in Frankfurt and also funded by the German Research Foundation) to investigate a p53 mutation called Y220C, which occurs in at least 30 cancer types and around 100,000 cancer patients every year.

This mutation makes p53 'wobbly' - meaning it can't do its job of protecting our cells. The team identified 'pockets' on the Y220C protein which potential drugs could connect to, along with ways to boost this connection. This work, along with research from other teams, laid the groundwork for new treatments that could work by stabilising the p53 Y220C mutant (see image showing the surface of the Y220C mutation with a small molecule stabilizer bound to it). By restoring the regular or 'wild type' version of the protein, treatments could reactivate p53’s protective functions in the mutated tumor cells, thereby stopping their unregulated growth and eventually killing them.

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