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Breast cancer is a widespread disease globally, and its occurrence has increased in many parts of the world over the past few decades. This has led to extensive research efforts aimed at finding better ways to treat it.
Scientists at AstraZeneca pursued a unique approach compared to other ongoing studies when developing drugs to target breast cancer that is specifically influenced by the hormone oestrogen. They utilised structure-based design (using macromolecular crystallography at Diamond), modelling, and Nuclear Magnetic Resonance (NMR) techniques to create a potent series of basic selective oestrogen receptor degraders (SERDs) antagonists with favourable chemical properties.
The primary goal of their study was to formulate an effective drug compound that did not affect hERG1 activity (a heart-related concern) and could be readily absorbed when taken orally.
1. A specific type of protein channel in the heart known as the human ether-a-go-go-related gene (hERG) potassium channel that plays a crucial role in regulating the electrical activity (rhythm) of the heart.
Diamond Light Source is the UK's national synchrotron science facility, located at the Harwell Science and Innovation Campus in Oxfordshire.
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