Cancer researchers at the University of Bath have measured systematically how efficient molecules are at suppressing the activity of a protein associated with prostate and other cancers. The molecules could eventually be developed into new anti-cancer drugs.
The research team from the Departments of Pharmacy & Pharmacology and Chemistry are studying a protein called α-methylacyl-CoA racemase (AMACR) as a potential target for cancer treatments. Levels of AMACR protein and activity are increased by ~10-fold in all prostate cancers. Reducing these levels using genetic techniques makes the cancer cells less aggressive, and their behaviour becomes more like normal cells.
Until relatively recently finding molecules that could target and inhibit AMACR has been challenging because it’s been difficult to accurately measure activity levels of the protein. However, after designing a simple colour-change test which can do precisely that, the University of Bath team were able to start analysing how the structure of promising molecules affects the activity of AMACR.
The team systematically varied the design of drug molecules in order to identify which parts of the molecule are important for effectiveness against AMACR.
In particular they confirmed that the ‘oiliness’ of a molecule is directly related to its potency – oily
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