Nanoformulation of BRD4-Degrading PROTAC: Improving Druggability To Target the ‘Undruggable’ MYC in Pancreatic Cancer

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Abstract

In a recent study, Saraswat and colleagues identified a novel proteolysis targeting chimera (PROTAC), ARV-825 (ARV), that efficiently degrades bromodomain-containing protein 4 (BRD4) to drug the ‘undruggable’ MYC in pancreatic cancer. ARV-loaded polyethylene glycol–poly lactic acid-co-glycolic acid (PLGA–PEG) polymeric nanoparticles (ARV-NPs) showed promising anticancer activity in both 2D cell culture and 3D multicellular tumor spheroid models of pancreatic cancer. This study demonstrates a unique therapeutic strategy in which targeting BRD4 for degradation via the E3 ubiquitin ligase cereblon (CRBN) pathway leads to sustained inhibition of oncogenic MYC expression for effective treatment of pancreatic cancer.

Original languageEnglish (US)
Pages (from-to)684-686
Number of pages3
JournalTrends in Pharmacological Sciences
Volume41
Issue number10
DOIs
StatePublished - Oct 2020

All Science Journal Classification (ASJC) codes

  • Toxicology
  • Pharmacology

Keywords

  • ARV-825
  • BRD4
  • MYC
  • PROTAC
  • pancreatic cancer
  • polymeric nanoparticles

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