dc.contributor.author | Liu, Xiaochuan | en_US |
dc.contributor.author | Wang, Aoli | en_US |
dc.contributor.author | Liang, Xiaofei | en_US |
dc.contributor.author | Chen, Cheng | en_US |
dc.contributor.author | Liu, Juanjuan | en_US |
dc.contributor.author | Zhao, Zheng | en_US |
dc.contributor.author | Wu, Hong | en_US |
dc.contributor.author | Deng, Yuanxin | en_US |
dc.contributor.author | Wang, Li | en_US |
dc.contributor.author | Wang, Beilei | en_US |
dc.contributor.author | Wu, Jiaxin | en_US |
dc.contributor.author | Liu, Feiyang | en_US |
dc.contributor.author | Fernandes, Stacey M. | en_US |
dc.contributor.author | Adamia, Sophia | en_US |
dc.contributor.author | Stone, Richard M. | en_US |
dc.contributor.author | Galinsky, Ilene A. | en_US |
dc.contributor.author | Brown, Jennifer R. | en_US |
dc.contributor.author | Griffin, James D. | en_US |
dc.contributor.author | Zhang, Shanchun | en_US |
dc.contributor.author | Loh, Teckpeng | en_US |
dc.contributor.author | Zhang, Xin | en_US |
dc.contributor.author | Wang, Wenchao | en_US |
dc.contributor.author | Weisberg, Ellen L. | en_US |
dc.contributor.author | Liu, Jing | en_US |
dc.contributor.author | Liu, Qingsong | en_US |
dc.date.accessioned | 2016-11-18T20:46:28Z | |
dc.date.issued | 2016 | en_US |
dc.identifier.citation | Liu, 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. | en |
dc.identifier.issn | 1949-2553 | en |
dc.identifier.uri | http://nrs.harvard.edu/urn-3:HUL.InstRepos:29408229 | |
dc.description.abstract | PI3Kδ 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. | en |
dc.language.iso | en_US | en |
dc.publisher | Impact Journals LLC | en |
dc.relation.isversionof | doi:10.18632/oncotarget.8702 | en |
dc.relation.hasversion | http://www.ncbi.nlm.nih.gov/pmc/articles/PMC5078040/pdf/ | en |
dash.license | LAA | en_US |
dc.subject | PI3Kδ | en |
dc.subject | leukemia | en |
dc.subject | B-cell malignances | en |
dc.subject | PI3K | en |
dc.subject | kinase inhibitors | en |
dc.title | Characterization of selective and potent PI3Kδ inhibitor (PI3KD-IN-015) for B-Cell malignances | en |
dc.type | Journal Article | en_US |
dc.description.version | Version of Record | en |
dc.relation.journal | Oncotarget | en |
dash.depositing.author | Adamia, Sophia | en_US |
dc.date.available | 2016-11-18T20:46:28Z | |
dc.identifier.doi | 10.18632/oncotarget.8702 | * |
dash.authorsordered | false | |
dash.contributor.affiliated | Adamia, Sophia | |
dash.contributor.affiliated | Griffin, James | |
dash.contributor.affiliated | Weisberg, Ellen | |
dash.contributor.affiliated | Brown, Jennifer | |
dash.contributor.affiliated | Stone, Richard | |