MODULATORS OF CULLIN 3 ADAPTOR KBTBD4 AS ANTI-CANCER COMPOUNDS
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Mar 9, 2023
app pub date -
Dec 18, 2020
filing date -
Dec 18, 2019
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It is provided the use of Pyrimido[4,5-B]indole derivatives as anti-cancer compounds, and more specifically the use of UM171 and its derivatives for treating cancer, by activating the CULLIN3-RING ubiquitin ligase complex which degrades RCOR1 which normally acts as the scaffolding protein for the RCOR1/LSD1 and HDAC2 complex, itself being dissociated in the presence of UM171. Thus UM171 acts like a molecular glue degrader, inhibiting HDACs, RCOR1, CoREST and LSD1 and resulting in an anti-cancer activity.
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