Article
A potent KRAS macromolecule degrader specifically targeting tumours with mutant KRAS.
Nature communications - 26 Jun 2020
Bery Nicolas, Miller Ami, Rabbitts Terry
Abstract excerpt
Tumour-associated KRAS mutations are the most prevalent in the three RAS-family isoforms and involve many different amino-acids. Therefore, molecules able to interfere with mutant KRAS protein are potentially important for wide-ranging tumour therapy. We describe the engineering of two RAS degraders based on protein macromolecules (macrodrugs) fused to specific E3 ligases. A KRAS-specific DARPin fused to the VHL...
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