KRAS-specific inhibition using a DARPin binding to a site in the allosteric lobe

KRAS-specific inhibition using a DARPin binding to a site in the allosteric lobe

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...

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Autores principales: 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
Formato: article
Lenguaje:EN
Publicado: Nature Portfolio 2019
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Science
Q
Acceso en línea:https://doaj.org/article/d60832bba2a448e1bd87fa3edb2b14fd
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Sumario: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.

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