Inhibition of RAS function through targeting an allosteric regulatory site

R Spencer-Smith, A Koide, Y Zhou, RR Eguchi… - Nature chemical …, 2017 - nature.com
R Spencer-Smith, A Koide, Y Zhou, RR Eguchi, F Sha, P Gajwani, D Santana, A Gupta
Nature chemical biology, 2017nature.com
RAS GTPases are important mediators of oncogenesis in humans. However,
pharmacological inhibition of RAS has proved challenging. Here we describe a functionally
critical region, located outside the effector lobe of RAS, that can be targeted for inhibition.
We developed NS1, a synthetic binding protein (monobody) that bound with high affinity to
both GTP-and GDP-bound states of H-RAS and K-RAS but not N-RAS. NS1 potently
inhibited growth factor signaling and oncogenic H-RAS-and K-RAS-mediated signaling and …
Abstract
RAS GTPases are important mediators of oncogenesis in humans. However, pharmacological inhibition of RAS has proved challenging. Here we describe a functionally critical region, located outside the effector lobe of RAS, that can be targeted for inhibition. We developed NS1, a synthetic binding protein (monobody) that bound with high affinity to both GTP- and GDP-bound states of H-RAS and K-RAS but not N-RAS. NS1 potently inhibited growth factor signaling and oncogenic H-RAS- and K-RAS-mediated signaling and transformation but did not block oncogenic N-RAS, BRAF or MEK1. NS1 bound the α4-β6-α5 region of RAS, which disrupted RAS dimerization and nanoclustering and led to blocking of CRAF–BRAF heterodimerization and activation. These results establish the importance of the α4-β6-α5 interface in RAS-mediated signaling and define a previously unrecognized site in RAS for inhibiting RAS function.
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