Targeting the canonical Wnt/β-catenin pathway in hematological malignancies

Cancer Sci. 2015 Jun;106(6):665-671. doi: 10.1111/cas.12655. Epub 2015 Apr 1.

Abstract

The canonical Wnt/β-catenin pathway plays an important role in different developmental processes through the regulation of stem cell functions. In the activation of the canonical Wnt/β-catenin pathway, β-catenin protein is imported into the nucleus and activates transcription of target genes including cyclin D1 and c-myc. Aberrant activation of the Wnt/β-catenin pathway contributes to carcinogenesis and malignant behaviors, and Wnt signaling is essential for the maintenance of cancer stem cells. The canonical Wnt/β-catenin pathway has been investigated extensively as a target in cancer treatment and several specific inhibitors of this signaling pathway have been identified through high-throughput screening. In this review, the significance of the canonical Wnt/β-catenin pathway in hematological carcinogenesis and screening methods for specific inhibitors are discussed.

Keywords: canonical Wnt pathway; hematological malignancies; high-throughput screening; small molecule inhibitors; β-Catenin.

Publication types

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

MeSH terms

  • Bone Marrow / physiology
  • Epigenesis, Genetic
  • Hematologic Neoplasms / drug therapy*
  • Hematologic Neoplasms / etiology
  • Hematologic Neoplasms / genetics
  • Humans
  • Neoplastic Stem Cells / physiology
  • Signal Transduction / drug effects
  • Signal Transduction / physiology
  • Wnt Signaling Pathway / drug effects*
  • Wnt Signaling Pathway / physiology
  • beta Catenin / antagonists & inhibitors*
  • beta Catenin / physiology

Substances

  • beta Catenin