Dipyridamole Inhibits Lipogenic Gene Expression by Retaining SCAP-SREBP in the Endoplasmic Reticulum

Ryan M. Esquejo, Manuel Roqueta-Rivera, Wei Shao, Peter E. Phelan, Uthpala Seneviratne, Christopher W. am Ende, Paul M. Hershberger, Carolyn E. Machamer, Peter J. Espenshade, Timothy F. Osborne

Research output: Contribution to journalArticlepeer-review

Abstract

Esquejo et al. report that dipyridamole, an FDA-approved anti-thrombotic phosphodiesterase (PDE) inhibitor, impedes endoplasmic reticulum to Golgi trafficking of sterol regulatory element-binding proteins (SREBPs) preventing their activation. A chemically modified version of dipyridamole that has no effect on PDE remains effective at SREBP blockage.

Original languageEnglish (US)
JournalCell Chemical Biology
DOIs
StateAccepted/In press - 2020

Keywords

  • cancer
  • cholesterol
  • gene expression
  • Insig
  • lipogenesis
  • obesity
  • repurposing dipyridamole
  • SCAP inhibitor
  • SREBP
  • triglycerides

ASJC Scopus subject areas

  • Biochemistry
  • Molecular Medicine
  • Molecular Biology
  • Pharmacology
  • Drug Discovery
  • Clinical Biochemistry

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