[PNAS]发现有效的SOS1抑制剂，通过破坏RAS-SOS1相互作用阻断RAS …
高通量和片段筛选的组合成功找到纳摩尔级别SOS1抑制剂，其有效地下调肿瘤细胞中的活性RAS。 在具有野生型 KRAS 的细胞中，我们观察到RAS-RAF-MEK-ERK途径的完全抑制。 在 …
SOS1 - Wikipedia
SOS1 is a guanine nucleotide exchange factor (GEF) which interacts with Ras proteins to phosphorylate GDP into GTP, or from an inactive state to an active state to signal cell …
Discovery of potent SOS1 inhibitors that block RAS activation …
2019年2月12日 · Here, we describe the identification of potent and cell-active small-molecule inhibitors which efficiently disrupt the interaction between KRAS and its exchange factor …
Discovery of potent SOS1 inhibitors that block RAS activation via ...
2019年1月25日 · This work describes a successful approach to identify nanomolar, selective, and cell-active inhibitors of SOS1, the exchange factor of RAS. The inhibitor design was enabled …
SOS signaling in RAS-mutated cancers - NCI - National Cancer …
2020年6月29日 · Understanding the mechanisms by which the ubiquitously expressed RasGEFs SOS1 and SOS2 promote WT RAS activation is an important step in determining the best …
Critical requirement of SOS1 RAS-GEF function for ... - Nature
2021年6月12日 · Our observations support a specific mechanistic link between SOS1 and control of intracellular redox homeostasis and mitochondrial function, and suggest that activation of …
SOS1 (son of sevenless 1) 作为RAS信号通路中的中心节点,可通过蛋白– 蛋白相互作用激活RAS 蛋白,因此SOS1 小分子抑制剂为治疗RAS依赖性癌症提供机遇。 最近一些文献和专利文件已 …
Allosteric nanobodies to study the interactions between SOS1 and RAS
2024年7月23日 · In this study, we exploited the unique properties of Nbs either to disrupt or to stabilize the SOS1 cat •KRAS G12V signaling complex (further referred to as SOS1•RAS) to …
SOS1 inhibitor BI-3406 shows in vivo antitumor activity akin to
These observations confirm SOS1 as an actionable therapy target in various RAS-dependent tumors and identify a therapeutic window for BI-3406-mediated SOS1 pharmacological …
综述 | Trends.Cancer | KRAS抑制剂：耐药驱动因素与联合策略
2024年12月27日 · 因此，抑制SOS1提供了一种潜在的泛RTK-RAS治疗策略。 SOS1抑制剂BI-3406与adagrasib联合使用导致肿瘤生长受损，即使是在由MRAS和SHOC2驱动的adagrasib …