Browsing by Author "Griffin, James"

Now showing items 1-8 of 8

    • 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, 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 ...

    • Kinase domain mutations confer resistance to novel inhibitors targeting JAK2V617F in myeloproliferative neoplasms 

      Deshpande, Anagha; Reddy, Mamatha M.; Schade, Georg O.M.; Ray, Arghya; Chowdary, Tirumala K.; Griffin, James D.; Sattler, Martin (2011)
      The transforming JAK2V617F kinase is frequently associated with myeloproliferative neoplasms (MPNs) and thought to be instrumental for the overproduction of myeloid lineage cells. Several small molecule drugs targeting ...

    • NADPH oxidases regulate cell growth and migration in myeloid cells transformed by oncogenic tyrosine kinases 

      Reddy, Mamatha M.; Fernandes, Margret S.; Salgia, Ravi; Levine, Ross L.; Griffin, James D.; Sattler, Martin (2014)
      Transformation by tyrosine kinase oncogenes in myeloid malignancies, including BCR-ABL in chronic myeloid leukemia, FLT3ITD in acute myeloid leukemia (AML) or JAK2V617F in myeloproliferative neoplasms (MPN), is associated ...

    • 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 ...

    • Structure of a pseudokinase domain switch that controls oncogenic activation of Jak kinases 

      Toms, Angela V.; Deshpande, Anagha; McNally, Randall; Jeong, Youngjee; Rogers, Julia M.; Kim, Chae Un; Gruner, Sol M.; Ficarro, Scott B.; Marto, Jarrod A.; Sattler, Martin; Griffin, James D.; Eck, Michael J. (2013)
      The V617F mutation in the Jak2 pseudokinase domain causes myeloproliferative neoplasms, and the equivalent mutation in Jak1 (V658F) is found in T-cell leukemias. Crystal structures of wild type and V658F mutant human Jak1 ...