Sareum’s Chk1 SAR-020106!26 Dec 2019 12:11
An Excellent Recent Research Publication on Sareum’s chk1 inhibitors used in combination!
Published: 21 October 2019
The Chk1 inhibitor SAR-020106 sensitizes human glioblastoma cells to irradiation, to temozolomide, and to decitabine treatment
“Our findings go along with recent reports of radiosensitization by these specific Chk1 inhibitors in human lung, colon, and head and neck cancer cell lines and xenograft models (SAR: [18, 21]; CCT244747: [55]). Human primary glioblastoma cells showed a similar dose-dependent radiosensitization by SAR confirming the relevance of the results found in glioblast- oma cell lines (Fig. 5e).”
Additional Combinations with AZN ATR Inhibitors!
“In the future, the here documented effects of the ChK1 inhibitor SAR might be further enhanced by addition of other mediators. For example, ATR inhibitors are already entering clinical trials and could inhibit ATR-mediated phosphorylation and activation of Chk1, thereby lowering the threshold for induction of cell death by Chk1 inhibitors”
Conclusion
Our data show that the inhibition of the S and the G2/ M checkpoint by SAR may synergize with therapeutic settings involving different DNA-damaging sources such as irradiation, TMZ, or decitabine. Thereby, the Chk1- specific inhibition by SAR provides an effective opportunity to target especially p53-defective tumour cells and exerts a low risk for neurotoxicities.
Full PDF & Article!
https://jeccr.biomedcentral.com/track/pdf/10.1186/s13046-019-1434-2
https://jeccr.biomedcentral.com/articles/10.1186/s13046-019-1434-2
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