Targeting protein kinase C-alpha (PKC-alpha) in cancer with the phosphorothioate antisense oligonucleotide aprinocarsen

Ann N Y Acad Sci. 2003 Dec;1002:263-70. doi: 10.1196/annals.1281.029.


Antisense oligonucleotides (ASOs) offer a novel pharmacological platform to develop highly specific drugs. As shown by the clinical development of aprinocarsen, an ASO directed against protein kinase C-alpha (PKC-alpha), this platform has made a remarkable advance from the bench to the bedside. This review summarizes the rationale of the early development of aprinocarsen and current clinical experience.

Publication types

  • Clinical Trial
  • Review

MeSH terms

  • Humans
  • Oligonucleotides, Antisense / pharmacology*
  • Protein Kinase C / antagonists & inhibitors*
  • Protein Kinase C / biosynthesis
  • Protein Kinase C / genetics
  • Protein Kinase C-alpha
  • RNA, Messenger / drug effects*


  • Oligonucleotides, Antisense
  • RNA, Messenger
  • PRKCA protein, human
  • Protein Kinase C
  • Protein Kinase C-alpha