Oxanthroquinone G01 is a potent inhibitor of KRAS and NRAS plasma membrane localization that potently inhibits proliferation of KRAS transformed cancer cells. Oxanthroquinone G01 also inhibits recycling of epidermal growth factor receptor and transferrin receptor, but has no influence on cholera toxin internalization. It also increases cellular levels of sphingomyelin and and ceramide.
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Chemical investigations of a soil-derived Streptomyces sp. led to the isolation of five new polyketides, (+)-oxanthromicin, (±)-hemi-oxanthromicins A/B, (±)-spiro-oxanthromicin A and oxanthroquinone, and the known alkaloid staurosporine, and the detection of four new metastable analogues, (±)-spiro-oxanthromicins B1/B2/C1/C2. Among the compounds
The Journal of biological chemistry, 293(35), 13696-13706 (2018-07-05)
Oncogenic RAS proteins are commonly expressed in human cancer. To be functional, RAS proteins must undergo post-translational modification and localize to the plasma membrane (PM). Therefore, compounds that prevent RAS PM targeting have potential as putative RAS inhibitors. Here we
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