Characterization of selective and potent PI3Kδ inhibitor (PI3KD-IN-015) for B-Cell malignances
Fernandes, Stacey M.
Galinsky, Ilene A.
Liu, QingsongNote: Order does not necessarily reflect citation order of authors.
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CitationLiu, X., A. Wang, X. Liang, C. Chen, J. Liu, Z. Zhao, H. Wu, et al. 2016. “Characterization of selective and potent PI3Kδ inhibitor (PI3KD-IN-015) for B-Cell malignances.” Oncotarget 7 (22): 32641-32651. doi:10.18632/oncotarget.8702. http://dx.doi.org/10.18632/oncotarget.8702.
AbstractPI3Kδ is predominately expressed in leukocytes and has been found overexpressed in B-cell related malignances such as CLL and AML. We have discovered a highly selective ATP competitive PI3Kd inhibitor PI3KD-IN-015, which exhibits a high selectivity among other PI3K isoforms in both biochemical assays and cellular assay, meanwhile did not inhibit most of other protein kinases in the kinome. PI3KD-IN-015 demonstrates moderately anti-proliferation efficacies against a variety of B-cell related cancer cell lines through down-regulate the PI3K signaling significantly. It induced both apoptosis and autophagy in B-cell malignant cell lines. In addition, combination of autophagy inhibitor Bafilomycin could potentiate the moderate anti-proliferation effect of PI3KD-IN-015. PI3KD-IN-015 shows anti-proliferation efficacy against CLL and AML patient primary cells. Collectively, these results indicate that PI3KD-IN-015 may be useful drug candidate for further development of anti-B-cell related malignances therapies.
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