2024
DOI: 10.1021/acs.jmedchem.3c01598
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A Potent SOS1 PROTAC Degrader with Synergistic Efficacy in Combination with KRASG12C Inhibitor

Yan Lv,
Zixuan Yang,
Yiming Chen
et al.

Abstract: AMG510, as the first approved inhibitor for KRAS G12C mutation, has shown promising efficacy in nonsmallcell lung cancer and colorectal cancer harboring KRAS G12C mutation. However, the moderate response rate and the rapid emergence of acquired resistance limit the therapeutic potential of AMG510, highlighting the need for the development of combination strategies. Here, we observed the suppression of RAS-MAPK signaling induced by AMG510 was prolonged and enhanced by SOS1 knockdown. Thus, we design, synthesize… Show more

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