A new family of drugs which inhibit the activity of a protein associated with prostate and other cancers has been reported by scientists from the University of Bath.
A new family of drugs which inhibit the activity of a protein associated with prostate and other cancers has been reported by scientists from the University of Bath.
They provide a promising avenue for research to potentially develop new therapies to treat a range of cancers thanks to the design of the study, which rationally investigates how the drugs work. The research team from the Departments of Pharmacy & Pharmacology and Chemistry study a protein called α-methylacyl-CoA racemase (AMACR). Levels of the AMACR protein and its activity are increased by ~10-fold in all prostate cancers, and a number of other cancers as well. Reducing levels of AMACR in prostate cancer cells using genetic techniques makes them less aggressive, and their behaviour becomes more like normal cells.
Until recently it was difficult to accurately measure AMACR activity and therefore hard to determine the effectiveness of drugs designed to reduce AMACR activity. This means that few studies on developing AMACR-targeted drugs had been carried out, and those that had been did not systematically investigate the structural features which contribute to high effectiveness. In this study a new family of drugs which inhibit AMACR is reported. The structure of the side-chain was systematically varied in order to identify important structural features which are required for highly effective inhibition of AMACR activity. This work resulted in a 20-fold increase in effectiveness in the drugs compared to those already known, such as ibuprofenoyl-CoA. The reported new drugs proved to work in a different way to ibuprofenoyl-CoA and similar drugs.
The study is published in the journal Bioorganic Chemistry.
Read more at University of Bath
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