Dual Specific Inhibitors Of The BCR-ABL and MNK Kinases As Potential Therapeutics For Blast Crisis Chronic Myeloid Leukemia

@article{Lim2013DualSI,
  title={Dual Specific Inhibitors Of The BCR-ABL and MNK Kinases As Potential Therapeutics For Blast Crisis Chronic Myeloid Leukemia},
  author={Sharon Xiaodai Lim and Joseph Cherian and Kassoum Nacro and Yun Shan Chew and Meng Ling Choong and Jun Li and Samantha Guo and Melvyn Ho and Joma Kanikadu Joy and Perlyn Zekui Kwek and May Ann Lee and Boping Liu and Vithya Manoharan and Esther H. Q. Ong and Vishal Pendharkar and Zhi Ying Poh and Anders Poulsen and Kanda Sangthongpitag and Kannan Srinivararaghavan and Siew Peng Tan and Haiyan Yang and Thomas Keller and Charles Chuah and Sin Tiong Ong and Jeffrey Hill and Alex Matter},
  journal={Blood},
  year={2013},
  volume={122},
  pages={2702-2702}
}
Pharmacologic inhibition of BCR-ABL by tyrosine kinase inhibitors (TKI) provides effective therapy for chronic phase but not blast crisis (BC) CML. The inability of TKIs to control BC CML is due to the reactivation of BCR-ABL through TKI resistance-conferring mutations, as well as the activation of alternative oncogenic pathways that mediate acquired leukemia stem cell (LSC) function and differentiation block in leukemic progenitors. Accordingly, the development of effective BC therapeutics… Expand
Structure-Activity Relationship Studies of Mitogen Activated Protein Kinase Interacting Kinase (MNK) 1 and 2 and BCR-ABL1 Inhibitors Targeting Chronic Myeloid Leukemic Cells.
TLDR
The identification of novel dual MNK1 and 2 and BCR-ABL1 inhibitors, starting from the known kinase inhibitor 2, which are efficacious in a mouse xenograft model and reduce the level of phosphorylated eukaryotic translation initiation factor 4E in the tumor tissues. Expand