Targeting few to help hundreds: JAK, MAPK and ROCK pathways as druggable targets in atypical chronic myeloid leukemia

Mol Cancer. 2018 Feb 19;17(1):40. doi: 10.1186/s12943-018-0774-4.

Abstract

Atypical Chronic Myeloid Leukemia (aCML) is a myeloproliferative neoplasm characterized by neutrophilic leukocytosis and dysgranulopoiesis. From a genetic point of view, aCML shows a heterogeneous mutational landscape with mutations affecting signal transduction proteins but also broad genetic modifiers and chromatin remodelers, making difficult to understand the molecular mechanisms causing the onset of the disease. The JAK-STAT, MAPK and ROCK pathways are known to be responsible for myeloproliferation in physiological conditions and to be aberrantly activated in myeloproliferative diseases. Furthermore, experimental evidences suggest the efficacy of inhibitors targeting these pathways in repressing myeloproliferation, opening the way to deep clinical investigations. However, the activation status of these pathways is rarely analyzed when genetic mutations do not occur in a component of the signaling cascade. Given that mutations in functionally unrelated genes give rise to the same pathology, it is tempting to speculate that alteration in the few signaling pathways mentioned above might be a common feature of pathological myeloproliferation. If so, targeted therapy would be an option to be considered for aCML patients.

Keywords: Atypical myeloid leukemia; CSF3R; Fasudil; JAK2; MAPK; ROCK; Ruxolitinib; Trametinib.

Publication types

  • Research Support, Non-U.S. Gov't
  • Review

MeSH terms

  • 1-(5-Isoquinolinesulfonyl)-2-Methylpiperazine / analogs & derivatives
  • 1-(5-Isoquinolinesulfonyl)-2-Methylpiperazine / therapeutic use
  • Animals
  • Humans
  • Janus Kinases / genetics
  • Janus Kinases / metabolism*
  • Leukemia, Myeloid, Chronic, Atypical, BCR-ABL Negative / drug therapy*
  • Leukemia, Myeloid, Chronic, Atypical, BCR-ABL Negative / metabolism*
  • Mitogen-Activated Protein Kinases / genetics
  • Mitogen-Activated Protein Kinases / metabolism*
  • Mutation / genetics
  • Nitriles
  • Pyrazoles / therapeutic use
  • Pyridones / therapeutic use
  • Pyrimidines
  • Pyrimidinones / therapeutic use
  • Signal Transduction / drug effects*
  • Signal Transduction / genetics
  • rho-Associated Kinases / genetics
  • rho-Associated Kinases / metabolism*

Substances

  • Nitriles
  • Pyrazoles
  • Pyridones
  • Pyrimidines
  • Pyrimidinones
  • trametinib
  • ruxolitinib
  • 1-(5-Isoquinolinesulfonyl)-2-Methylpiperazine
  • Janus Kinases
  • rho-Associated Kinases
  • Mitogen-Activated Protein Kinases
  • fasudil