KRAS-specific inhibition using a DARPin binding to a site in the allosteric lobe
oleh: Nicolas Bery, Sandrine Legg, Judit Debreczeni, Jason Breed, Kevin Embrey, Christopher Stubbs, Paulina Kolasinska-Zwierz, Nathalie Barrett, Rose Marwood, Jo Watson, Jon Tart, Ross Overman, Ami Miller, Christopher Phillips, Ralph Minter, Terence H. Rabbitts
| Format: | Article |
|---|---|
| Diterbitkan: | Nature Portfolio 2019-06-01 |
Deskripsi
Mutant RAS family members occur in a wide range of tumour types, and there is a great interest in identifying isoform-specific inhibitors. Here, the authors characterise two designed ankyrin repeat proteins (DARPins) that specifically inhibit the KRAS isoform by binding to the region around the KRAS-specific residue histidine 95 and show that they affect KRAS/effector interactions in different ways.