Completed Cancer Chemistry

Cancer Medicines Discovery II

In plain English

AI plain-English summary

A team in Leeds is designing small-molecule drugs that either activate a tumour-killing enzyme or block a protein that helps cancer cells spread. This matters because many cancers become resistant to existing treatments or spread to other parts of the body, where they become much harder to treat. The researchers are targeting two specific biological mechanisms. The first uses enzymes called cytochromes P450, which are more active inside tumours than in healthy tissue, to selectively activate a toxic drug only in cancer cells. The second targets polysialyltransferases, enzymes that help tumour cells migrate and grow. If the programme succeeds, it will produce preclinical proof-of-concept drugs ready for further development and eventual clinical trials. This could lead to new treatment options for patients whose cancers have limited therapies, particularly those with aggressive or metastatic disease. The work builds on earlier milestones in target identification and druggability, and the group has a track record of moving discoveries from the lab into human trials.

View original technical description
This translational research programme will progress, to preclinical proof‐of concept (PoC) small‐molecule drugs against novel cancer targets. The work will be progressed by a multidisciplinary group with a track‐record in new drug discovery from concept through development and into clinical trials with clinical colleagues in Leeds. The work is focused on two therapeutic strategies that require a common approach for their progression: (i) tumour‐selective cytotoxic drug activation by cytochromes P450 (CYPs) with elevated activity within the tumour microenvironment, (ii) inhibition of tumour migration, growth and progression through targeting of polysialyltransferases (PST and STX). The programme will build upon important milestones previously achieved that relate to target identification, druggability and progression towards PoC.

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Researchers

Robert Falconer (EPMC Awardee)

Related Research

Grants with similar aims, by meaning.

Cancer Research UK Cancer Therapeutics Unit
The Cancer Research UK Drug Discovery Programme at the Newcastle Cancer Centre, Newcastle University
Support for Cancer Medicine Discovery at the Institute of Cancer Therapeutics
Small Molecule Cancer Drug Discovery Programme Grant
Protein lipidation in cancer: discovery, mechanisms and target validation

Original classification

Research Grant

Plain English summaries and category classifications on this site are generated by AI and may not perfectly reflect the original research.