Issue 40

Creu er mwyn dinistrio: Creu rhyngolyn GN8 anghymesur i drin clefydau prion (Create in order to destroy: synthesis of an unsymmetrical GN8 intermediate to treat prion diseases)

In this paper, we have prepared a strong foundation to synthesise PROTACs in order to target the prion protein. Computational chemistry was used to generate a postulated binding mode to suggest a linker attachment point. Following this, a key unsymmetrical GN8 intermediate was designed and synthesised that will be used in the future to react with linker-E3 ligase reactants to create the first ever prion targeting PROTACs.

Keywords

PROTAC, Prion Diseases, Medicinal Chemistry, GN8.

Reference

Thomas, B., Ward, S., Jones, H., (2025), ‘Creu er mwyn dinistrio: Creu rhyngolyn GN8 anghymesur i drin clefydau prion’, Gwerddon, 40, 49–65. https://doi.org/10.61257/GWER4003

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