Inhibitor of Wnt/β-catenin and Ras pathways by enhancing formation of the β-catenin destruction complex
KYA1797K is an inhibitor of both Wnt/β-catenin and Ras pathways. It binds to the axin regulators of the G-protein signaling (RGS) domain enhancing formation of the β-catenin destruction complex and inducing activation GSK3β, which results in phosphorylation and subsequent degradation of both β-catenin and K-Ras. KYA1797K was show to suppress tumor growth and progression in mouse xenografts of CRC cells that had APC and K-Ras mutations.
Nature chemical biology, 12(8), 593-600 (2016-06-14)
Both the Wnt/β-catenin and Ras pathways are aberrantly activated in most human colorectal cancers (CRCs) and interact cooperatively in tumor promotion. Inhibition of these signaling may therefore be an ideal strategy for treating CRC. We identified KY1220, a compound that
In order to efficiently produce infectious viral particles, HIV must counter several restrictions exerted by host cell antiviral proteins. MARCH1 is a member of the MARCH protein family that restricts HIV infection by limiting the incorporation of viral envelope glycoproteins
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