PHLPPs: Emerging players in metabolic disorders

Drug Discov Today. 2022 Oct;27(10):103317. doi: 10.1016/j.drudis.2022.07.002. Epub 2022 Jul 11.

Abstract

That reversible protein phosphorylation by kinases and phosphatases occurs in metabolic disorders is well known. Various studies have revealed that a multi-faceted and tightly regulated phosphatase, pleckstrin homology domain leucine-rich repeat protein phosphatase (PHLPP)-1/2 displays robust effects in cardioprotection, ischaemia/reperfusion (I/R), and vascular remodelling. PHLPP1 promotes foamy macrophage development through ChREBP/AMPK-dependent pathways. Adipocyte-specific loss of PHLPP2 reduces adiposity, improves glucose tolerance,and attenuates fatty liver via the PHLPP2-HSL-PPARα axis. Discoveries of PHLPP1-mediated insulin resistance and pancreatic β cell death via the PHLPP1/2-Mst1-mTORC1 triangular loop have shed light on its significance in diabetology. PHLPP1 downregulation attenuates diabetic cardiomyopathy (DCM) by restoring PI3K-Akt-mTOR signalling. In this review, we summarise the functional role of, and cellular signalling mediated by, PHLPPs in metabolic tissues and discuss their potential as therapeutic targets.

Keywords: Atherosclerosis; Cardiovascular dysfunction; PHLPP1; PHLPP2; Type 2 diabetes.

Publication types

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

MeSH terms

  • AMP-Activated Protein Kinases
  • Glucose
  • Humans
  • Insulin Resistance*
  • Mechanistic Target of Rapamycin Complex 1
  • Nuclear Proteins / metabolism
  • PPAR alpha
  • Phosphatidylinositol 3-Kinases
  • Phosphoprotein Phosphatases* / metabolism
  • Proto-Oncogene Proteins c-akt / metabolism
  • TOR Serine-Threonine Kinases

Substances

  • Nuclear Proteins
  • PPAR alpha
  • Mechanistic Target of Rapamycin Complex 1
  • Proto-Oncogene Proteins c-akt
  • TOR Serine-Threonine Kinases
  • AMP-Activated Protein Kinases
  • PHLPP2 protein, human
  • Phosphoprotein Phosphatases
  • Glucose