4.6 Review

All roads lead to PP2A: exploiting the therapeutic potential of this phosphatase

Journal

FEBS JOURNAL
Volume 283, Issue 6, Pages 1004-1024

Publisher

WILEY
DOI: 10.1111/febs.13573

Keywords

cancer; cancer biology; cell signaling; CIP2A; drug development; PP2A; protein phosphatases; SET; structural biology; tumor suppressors

Funding

  1. Howard Hughes Medical Institute (HHMI) Physician-Scientist Early Career Award
  2. Case Comprehensive Cancer Center Pilot Award
  3. NCI [R01CA181654]

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Protein phosphatase 2A (PP2A) is a serine/ threonine phosphatase involved in the regulation of many cellular processes. A confirmed tumor suppressor protein, PP2A is genetically altered or functionally inactivated in many cancers highlighting a need for its therapeutic reactivation. In this review we discuss recent literature on PP2A: the elucidation of its structure and the functions of its subunits, and the identification of molecular lesions and post-translational modifications leading to its dysregulation in cancer. A final section will discuss the proteins and small molecules that modulate PP2A and how these might be used to target dysregulated forms of PP2A to treat cancers and other diseases.

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