Chemistry:VUBI1
From HandWiki
VUBI1 is a drug that acts as an activator of the guanine nucleotide exchange factor protein SOS1, increasing the rate at which it catalyzes the exchange of GDP for GTP on its target protein KRAS. While inhibitors of SOS1 have been more widely researched for the treatment of cancer, under some conditions increasing SOS1 activity can also have an anti-cancer effect by destructive overactivation of cellular signaling processes, so SOS1 activators are also of potential clinical interest, as well as being used for the study of the SOS1-KRAS intercellular pathway.[1][2]
References
- ↑ "Discovery and Structure-Based Optimization of Benzimidazole-Derived Activators of SOS1-Mediated Nucleotide Exchange on RAS". Journal of Medicinal Chemistry 61 (19): 8875–8894. October 2018. doi:10.1021/acs.jmedchem.8b01108. PMID 30205005.
- ↑ "Targeting of SOS1: from SOS1 Activators to Proteolysis Targeting Chimeras". Current Pharmaceutical Design 29 (22): 1741–1746. 2023. doi:10.2174/1381612829666230418114520. PMID 37073657.
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