Now showing items 1-7 of 7

    • Characterization of selective and potent PI3Kδ inhibitor (PI3KD-IN-015) for B-Cell malignances 

      Liu, Xiaochuan; Wang, Aoli; Liang, Xiaofei; Chen, Cheng; Liu, Juanjuan; Zhao, Zheng; Wu, Hong; Deng, Yuanxin; Wang, Li; Wang, Beilei; Wu, Jiaxin; Liu, Feiyang; Fernandes, Stacey M.; Adamia, Sophia; Stone, Richard M.; Galinsky, Ilene A.; Brown, Jennifer R.; Griffin, James D.; Zhang, Shanchun; Loh, Teckpeng; Zhang, Xin; Wang, Wenchao; Weisberg, Ellen L.; Liu, Jing; Liu, Qingsong (Impact Journals LLC, 2016)
      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 ...
    • Discovery of a Potent and Selective DDR1 Receptor Tyrosine Kinase Inhibitor 

      Kim, Hyung-Gu; Tan, Li; Weisberg, Ellen L.; Liu, Feiyang; Canning, Peter; Choi, Hwan Geun; Ezell, Scott A.; Wu, Hong; Zhao, Zheng; Wang, Jinhua; Mandinova, Anna; Griffin, James D.; Bullock, Alex N.; Liu, Qingsong; Lee, Sam W.; Gray, Nathanael S. (American Chemical Society, 2013)
      The DDR1 receptor tyrosine kinase is activated by matrix collagens and has been implicated in numerous cellular functions such as proliferation, differentiation, adhesion, migration, and invasion. Here we report the discovery ...
    • Discovery of a Potent, Covalent BTK Inhibitor for B-Cell Lymphoma 

      Wu, Hong; Wang, Wenchao; Liu, Feiyang; Weisberg, Ellen L.; Tian, Bei; Chen, Yongfei; Li, Binhua; Wang, Aoli; Wang, Beilei; Zhao, Zheng; McMillin, Douglas W.; Hu, Chen; Li, Hong; Wang, Jinhua; Liang, Yanke; Buhrlage, Sara J.; Liang, Junting; Liu, Jing; Yang, Guang; Brown, Jennifer R.; Treon, Steven P.; Mitsiades, Constantine S.; Griffin, James D.; Liu, Qingsong; Gray, Nathanael S. (American Chemical Society, 2014)
      BTK is a member of the TEC family of non-receptor tyrosine kinases whose deregulation has been implicated in a variety of B-cell-related diseases. We have used structure-based drug design in conjunction with kinome profiling ...
    • Dual inhibition of AKT/FLT3-ITD by A674563 overcomes FLT3 ligand-induced drug resistance in FLT3-ITD positive AML 

      Wang, Aoli; Wu, Hong; Chen, Cheng; Hu, Chen; Qi, Ziping; Wang, Wenchao; Yu, Kailin; Liu, Xiaochuan; Zou, Fengming; Zhao, Zheng; Wu, Jiaxin; Liu, Juan; Liu, Feiyang; Wang, Li; Stone, Richard M.; Galinksy, Ilene A.; Griffin, James D.; Zhang, Shanchun; Weisberg, Ellen L.; Liu, Jing; Liu, Qingsong (Impact Journals LLC, 2016)
      The FLT3-ITD mutation is one of the most prevalent oncogenic mutations in AML. Several FLT3 kinase inhibitors have shown impressive activity in clinical evaluation, however clinical responses are usually transient and ...
    • Ibrutinib selectively and irreversibly targets EGFR (L858R, Del19) mutant but is moderately resistant to EGFR (T790M) mutant NSCLC Cells 

      Wu, Hong; Wang, Aoli; Zhang, Wei; Wang, Beilei; Chen, Cheng; Wang, Wenchao; Hu, Chen; Ye, Zi; Zhao, Zheng; Wang, Li; Li, Xixiang; Yu, Kailin; Liu, Juan; Wu, Jiaxin; Yan, Xiao-E; Zhao, Peng; Wang, Jinhua; Wang, Chu; Weisberg, Ellen L.; Gray, Nathanael S.; Yun, Cai-Hong; Liu, Jing; Chen, Liang; Liu, Qingsong (Impact Journals LLC, 2015)
      Through comprehensive comparison study, we found that ibrutinib, a clinically approved covalent BTK kinase inhibitor, was highly active against EGFR (L858R, del19) mutant driven NSCLC cells, but moderately active to the ...
    • Pathological glycogenesis through glycogen synthase 1 and suppression of excessive AMP kinase activity in myeloid leukemia cells 

      Bhanot, Haymanti; Reddy, Mamatha M.; Nonami, Atsushi; Weisberg, Ellen L.; Bonal, Dennis; Kirschmeier, Paul T.; Salgia, Sabrina; Podar, Klaus; Galinsky, Ilene; Chowdary, Tirumala K.; Neuberg, Donna; Tonon, Giovanni; Stone, Richard M.; Asara, John; Griffin, James D.; Sattler, Martin (2015)
      The rapid proliferation of myeloid leukemia cells is highly dependent on increased glucose metabolism. Through an unbiased metabolomics analysis of leukemia cells, we found that the glycogenic precursor UDP-D-glucose is ...
    • Selective Akt Inhibitors Synergize with Tyrosine Kinase Inhibitors and Effectively Override Stroma-Associated Cytoprotection of Mutant FLT3-Positive AML Cells 

      Weisberg, Ellen; Liu, Qingsong; Zhang, Xin; Nelson, Erik; Sattler, Martin; Liu, Feiyang; Nicolais, Maria; Zhang, Jianming; Mitsiades, Constantine S; Smith, Robert Walsh; Stone, Richard; Galinsky, Ilene; Nonami, Atsushi; Griffin, James D.; Gray, Nathanael (Public Library of Science, 2013)
      Objectives: Tyrosine kinase inhibitor (TKI)-treated acute myeloid leukemia (AML) patients commonly show rapid and significant peripheral blood blast cell reduction, however a marginal decrease in bone marrow blasts. This ...