Modulation of serine/threonine-protein phosphatase 1 (PP1) complexes: A promising approach in cancer treatment

Drug Discov Today. 2021 Nov;26(11):2680-2698. doi: 10.1016/j.drudis.2021.08.001. Epub 2021 Aug 12.

Abstract

Cancer is the second leading cause of death worldwide. Despite the availability of numerous therapeutic options, tumor heterogeneity and chemoresistance have limited the success of these treatments, and the development of effective anticancer therapies remains a major focus in oncology research. The serine/threonine-protein phosphatase 1 (PP1) and its complexes have been recognized as potential drug targets. Research on the modulation of PP1 complexes is currently at an early stage, but has immense potential. Chemically diverse compounds have been developed to disrupt or stabilize different PP1 complexes in various cancer types, with the objective of inhibiting disease progression. Beneficial results obtained in vitro now require further pre-clinical and clinical validation. In conclusion, the modulation of PP1 complexes seems to be a promising, albeit challenging, therapeutic strategy for cancer.

Keywords: Cancer treatment; PP1 complexes; Peptides; Small molecules.

Publication types

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

MeSH terms

  • Humans
  • Multiprotein Complexes / metabolism*
  • Neoplasms / drug therapy*
  • Neoplasms / metabolism
  • Protein Phosphatase 1 / metabolism*

Substances

  • Multiprotein Complexes
  • Protein Phosphatase 1