Proteinkinase C-β Inhibitors sensitise Malignant B Cells To Cytotoxic Drugs
Lutzny G, Li Z, Oelsner M, et al.




Key Points:
  • Authors aim to show PKC-β inhibitor (enzastaurin) potentiates cytotoxic effects of ABT737 in synergistic manner
  • PKC-β deficient stromal cells fail to maintain high expression levels of anti-apoptotic proteins
  • They show significantly enhanced sensitivity to ABT737 compared to CLL cells cultured on PKC-β proficient stromal cells
  • In vivo studies in mice demonstrated combination of enzastaurin and ABT199 superior to single agent treatment, when assessed by PET-CT scan
Implications:

  • PKC-β inhibitor enzastaurin enhances cytotoxic effects of standard chemotherapeutic drugs and of BCL2-inhibitor ABT737

View the original abstract on the ASH website.






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