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WNT-TCF response blockade by a small molecules

ABSTRACT: WNT-TCF response blockade by a small molecules

PROVIDER: PRJNA347984 | ENA |

REPOSITORIES: ENA

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Long-lasting WNT-TCF response blocking and epigenetic modifying activities of withanolide F in human cancer cells

Project description:The WNT-TCF signaling pathway participates in adult tissue homeostasis and repair, and is hyperactive in a number of human diseases including cancers of the colon. Whereas to date there are no antagonists approved for patient use, a potential problem for their sustained use is the blockade of WNT signaling in healthy tissues, thus provoking potentially serious co-lateral damage. Here we have screened a library of plant and microorganism small molecules for novel WNT signaling antagonists and describe withanolide F as a potent WNT-TCF response blocker. This steroidal lactone inhibits TCF-dependent colon cancer xenograft growth and mimics the effects of genetic blockade of TCF and of ivermectin, a previously reported WNT-TCF blocker. However, withanolide F is unique in that it imposes a long-lasting repression of tumor growth, WNT-TCF targets and cancer stem cell clonogenicity long after drug treatment

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WNT-TCF response blockade by a small molecules

Project description:This SuperSeries is composed of the SubSeries listed below.

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TCF/LEF dependent and independent regulation of Wnt/beta-catenin transcription

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