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Association details:
| Biomarker: | KRAS G12D |
|---|---|
| Cancer: | Colorectal Cancer |
| Drug: | Ibrance (palbociclib) (CDK4 inhibitor, CDK6 inhibitor) + MSC2504877 (TNKS inhibitor) |
| Direction: | Resistant |
Evidence:
Source:
Title:
A novel tankyrase inhibitor, MSC2504877, enhances the effects of clinical CDK4/6 inhibitors
Published date:
01/19/2019
Excerpt:
Here, we describe here a novel, drug-like small molecule inhibitor of tankyrase MSC2504877 that inhibits the growth of APC mutant colorectal tumour cells...However, the presence of an oncogenic Kras p.G12D mutation in mice reversed the effects of the MSC2504877/palbociclib combination, suggesting one molecular route that could lead to drug resistance.…we found the presence of the KRasG12D mutation reversed the inhibitory effects of the MSC2504877 + palbociclib combination.
DOI:
10.1038/s41598-018-36447-4
