Characterization of selective and potent PI3K delta inhibitor (PI3KD-IN-015) for B-Cell malignances

doi:10.18632/oncotarget.8702

CORC > 合肥物质科学研究院 > 中国科学院合肥物质科学研究院 > 中科院强磁场科学中心

	Characterization of selective and potent PI3K delta inhibitor (PI3KD-IN-015) for B-Cell malignances
	Liu, Xiaochuan 1,2; Wang, Aoli 2,3; Liang, Xiaofei 2,4; Chen, Cheng 2,4; Liu, Juanjuan 2,3; Zhao, Zheng 2,4; Wu, Hong 2,3; Deng, Yuanxin 2,3; Wang, Li 2,4; Wang, Beilei 2,4
刊名	ONCOTARGET
	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
内容类型	期刊论文
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.