Characterization of selective and potent PI3K delta inhibitor (PI3KD-IN-015) for B-Cell malignances
文献类型:期刊论文
作者 | Liu, Xiaochuan1,2![]() ![]() ![]() ![]() ![]() |
刊名 | ONCOTARGET
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出版日期 | 2016-05-31 |
卷号 | 7期号:22页码:32641-32651 |
关键词 | Pi3k Delta Leukemia B-cell Malignances Pi3k Kinase Inhibitors |
DOI | 10.18632/oncotarget.8702 |
文献子类 | Article |
英文摘要 | PI3K delta 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 PI3K delta 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 antiproliferation 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. |
WOS关键词 | CHRONIC LYMPHOCYTIC-LEUKEMIA ; PI3K ; P110-DELTA ; IDELALISIB ; 3-KINASES ; SURVIVAL ; ISOFORM ; CANCER |
WOS研究方向 | Oncology ; Cell Biology |
语种 | 英语 |
WOS记录号 | WOS:000377748500078 |
资助机构 | Chinese Academy of Sciences ; Chinese Academy of Sciences ; Chinese Academy of Sciences ; Chinese Academy of Sciences ; Chinese Academy of Sciences ; Chinese Academy of Sciences ; Chinese Academy of Sciences ; Chinese Academy of Sciences ; Anhui Province Natural Science Foundation Annual Key Program(1301023011) ; Anhui Province Natural Science Foundation Annual Key Program(1301023011) ; Anhui Province Natural Science Foundation Annual Key Program(1301023011) ; Anhui Province Natural Science Foundation Annual Key Program(1301023011) ; Anhui Province Natural Science Foundation Annual Key Program(1301023011) ; Anhui Province Natural Science Foundation Annual Key Program(1301023011) ; Anhui Province Natural Science Foundation Annual Key Program(1301023011) ; Anhui Province Natural Science Foundation Annual Key Program(1301023011) ; China "Thousand Talents Program" ; China "Thousand Talents Program" ; China "Thousand Talents Program" ; China "Thousand Talents Program" ; China "Thousand Talents Program" ; China "Thousand Talents Program" ; China "Thousand Talents Program" ; China "Thousand Talents Program" ; "Hundred Talents Program" of The Chinese Academy of Sciences ; "Hundred Talents Program" of The Chinese Academy of Sciences ; "Hundred Talents Program" of The Chinese Academy of Sciences ; "Hundred Talents Program" of The Chinese Academy of Sciences ; "Hundred Talents Program" of The Chinese Academy of Sciences ; "Hundred Talents Program" of The Chinese Academy of Sciences ; "Hundred Talents Program" of The Chinese Academy of Sciences ; "Hundred Talents Program" of The Chinese Academy of Sciences ; Scientific Research Grant of Hefei Science Center of CAS (SRG-HSC)(2015SRG-HSC022) ; Scientific Research Grant of Hefei Science Center of CAS (SRG-HSC)(2015SRG-HSC022) ; Scientific Research Grant of Hefei Science Center of CAS (SRG-HSC)(2015SRG-HSC022) ; Scientific Research Grant of Hefei Science Center of CAS (SRG-HSC)(2015SRG-HSC022) ; Scientific Research Grant of Hefei Science Center of CAS (SRG-HSC)(2015SRG-HSC022) ; Scientific Research Grant of Hefei Science Center of CAS (SRG-HSC)(2015SRG-HSC022) ; Scientific Research Grant of Hefei Science Center of CAS (SRG-HSC)(2015SRG-HSC022) ; Scientific Research Grant of Hefei Science Center of CAS (SRG-HSC)(2015SRG-HSC022) ; CAS/SAFEA international partnership program for creative research teams ; CAS/SAFEA international partnership program for creative research teams ; CAS/SAFEA international partnership program for creative research teams ; CAS/SAFEA international partnership program for creative research teams ; CAS/SAFEA international partnership program for creative research teams ; CAS/SAFEA international partnership program for creative research teams ; CAS/SAFEA international partnership program for creative research teams ; CAS/SAFEA international partnership program for creative research teams ; Chinese Academy of Sciences ; Chinese Academy of Sciences ; Chinese Academy of Sciences ; Chinese Academy of Sciences ; Chinese Academy of Sciences ; Chinese Academy of Sciences ; Chinese Academy of Sciences ; Chinese Academy of Sciences ; Anhui Province Natural Science Foundation Annual Key Program(1301023011) ; Anhui Province Natural Science Foundation Annual Key Program(1301023011) ; Anhui Province Natural Science Foundation Annual Key Program(1301023011) ; Anhui Province Natural Science Foundation Annual Key Program(1301023011) ; Anhui Province Natural Science Foundation Annual Key Program(1301023011) ; Anhui Province Natural Science Foundation Annual Key Program(1301023011) ; Anhui Province Natural Science Foundation Annual Key Program(1301023011) ; Anhui Province Natural Science Foundation Annual Key Program(1301023011) ; China "Thousand Talents Program" ; China "Thousand Talents Program" ; China "Thousand Talents Program" ; China "Thousand Talents Program" ; China "Thousand Talents Program" ; China "Thousand Talents Program" ; China "Thousand Talents Program" ; China "Thousand Talents Program" ; "Hundred Talents Program" of The Chinese Academy of Sciences ; "Hundred Talents Program" of The Chinese Academy of Sciences ; "Hundred Talents Program" of The Chinese Academy of Sciences ; "Hundred Talents Program" of The Chinese Academy of Sciences ; "Hundred Talents Program" of The Chinese Academy of Sciences ; "Hundred Talents Program" of The Chinese Academy of Sciences ; "Hundred Talents Program" of The Chinese Academy of Sciences ; "Hundred Talents Program" of The Chinese Academy of Sciences ; Scientific Research Grant of Hefei Science Center of CAS (SRG-HSC)(2015SRG-HSC022) ; Scientific Research Grant of Hefei Science Center of CAS (SRG-HSC)(2015SRG-HSC022) ; Scientific Research Grant of Hefei Science Center of CAS (SRG-HSC)(2015SRG-HSC022) ; Scientific Research Grant of Hefei Science Center of CAS (SRG-HSC)(2015SRG-HSC022) ; Scientific Research Grant of Hefei Science Center of CAS (SRG-HSC)(2015SRG-HSC022) ; Scientific Research Grant of Hefei Science Center of CAS (SRG-HSC)(2015SRG-HSC022) ; Scientific Research Grant of Hefei Science Center of CAS (SRG-HSC)(2015SRG-HSC022) ; Scientific Research Grant of Hefei Science Center of CAS (SRG-HSC)(2015SRG-HSC022) ; CAS/SAFEA international partnership program for creative research teams ; CAS/SAFEA international partnership program for creative research teams ; CAS/SAFEA international partnership program for creative research teams ; CAS/SAFEA international partnership program for creative research teams ; CAS/SAFEA international partnership program for creative research teams ; CAS/SAFEA international partnership program for creative research teams ; CAS/SAFEA international partnership program for creative research teams ; CAS/SAFEA international partnership program for creative research teams |
源URL | [http://ir.hfcas.ac.cn:8080/handle/334002/22446] ![]() |
专题 | 合肥物质科学研究院_中科院强磁场科学中心 |
作者单位 | 1.Univ Sci & Technol China, Dept Chem, Hefei 230036, Anhui, Peoples R China 2.Chinese Acad Sci, High Field Magnet Lab, Hefei 230031, Anhui, Peoples R China 3.Univ Sci & Technol China, Hefei 230036, Anhui, Peoples R China 4.CHMFL HCMTC Target Therapy Joint Lab, Hefei 230031, Anhui, Peoples R China 5.Harvard Univ, Sch Med, Dana Farber Canc Inst, Dept Med Oncol, 44 Binney St, Boston, MA 02115 USA 6.Hefei Cosource Med Technol Co LTD, Hefei 230031, Anhui, Peoples R China 7.Chinese Acad Sci, Hefei Sci Ctr, Hefei 230031, Anhui, Peoples R China |
推荐引用方式 GB/T 7714 | Liu, Xiaochuan,Wang, Aoli,Liang, Xiaofei,et al. Characterization of selective and potent PI3K delta inhibitor (PI3KD-IN-015) for B-Cell malignances[J]. ONCOTARGET,2016,7(22):32641-32651. |
APA | Liu, Xiaochuan.,Wang, Aoli.,Liang, Xiaofei.,Chen, Cheng.,Liu, Juanjuan.,...&Liu, Qingsong.(2016).Characterization of selective and potent PI3K delta inhibitor (PI3KD-IN-015) for B-Cell malignances.ONCOTARGET,7(22),32641-32651. |
MLA | Liu, Xiaochuan,et al."Characterization of selective and potent PI3K delta inhibitor (PI3KD-IN-015) for B-Cell malignances".ONCOTARGET 7.22(2016):32641-32651. |
入库方式: OAI收割
来源:合肥物质科学研究院
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