Introducing a photoaffinity labelling (PAL) probe to biological systems can bring many benefits, enabling users to identify new drug targets and binding sites. Using this method, scientists can characterise even weak or transient protein-ligand interactions of small molecules, for both on- and off- target binding.
Designing efficient PAL probes is very challenging, however, a group of scientists from GSK has recently used Macromolecular Crystallography (MX) at Diamond, to explore the stability and effectiveness of a range of probes containing various photoreactive groups. A Ugi protocol was identified as an effective means to synthesise a range of PAL probes in a single step.
The long-term aim of this study is to reduce attrition rates for candidate drug molecules in clinical trials.
To find out what the team discovered, read the publication.
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