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Total 78 results found since Jan 2013.
Creation of a new class of radiosensitizers for glioblastoma based on the mibefradil pharmacophore
We present in vivo pharmacokinetic studies of the top analogues with evidence of brain penetration. We also report a targeted siRNA-based screen which suggests a possible role for mTOR and Akt in DNA repair inhibition by this class of drugs. Taken together, these data reveal a new class of mibefradil-based DNA repair inhibitors which can be further advanced into pre-clinical testing and eventually clinical trials, as potential GBM radiosensitizers.PMID:33953843 | PMC:PMC8092340 | DOI:10.18632/oncotarget.27933
Source: Oncotarget - May 6, 2021 Category: Cancer & Oncology Authors: Sateja Paradkar James Herrington Adam Hendricson Piyasena Hewawasam Mark Plummer Denton Hoyer Ranjini K Sundaram Yulia V Surovtseva Ranjit S Bindra Source Type: research
Cancers, Vol. 15, Pages 3432: Vitamin D Receptor Antagonist MeTC7 Inhibits PD-L1
In this study, using chromatin immunoprecipitation (ChIP) assay and siRNA, we demonstrate that vitamin D/VDR regulates PD-L1 expression in acute myeloid leukemia (AML) and myelodysplastic syndrome (MDS) cells. We have examined whether a VDR antagonist, MeTC7, can inhibit PD-L1. To ensure that MeTC7 inhibits VDR/PD-L1 without off-target effects, we examined competitive inhibition of VDR by MeTC7, utilizing ligand-dependent dimerization of VDR-RXR, RXR-RXR, and VDR-coactivators in a mammalian 2-hybrid (M2H) assay. MeTC7 inhibits VDR selectively, suppresses PD-L1 expression sparing PD-L2, and inhibits the cell viability, clon...
Source: Cancers - June 30, 2023 Category: Cancer & Oncology Authors: Negar Khazan Emily R. Quarato Niloy A. Singh Cameron W. A. Snyder Taylor Moore John P. Miller Masato Yasui Yuki Teramoto Takuro Goto Sabeeha Reshi Jennifer Hong Naixin Zhang Diya Pandey Priyanka Srivastava Alexandra Morell Hiroki Kawano Yuko Kawano Thomas Tags: Article Source Type: research
