The role of protein kinase C-alpha (PKC-alpha) in cancer and its modulation by the novel PKC-alpha-specific inhibitor aprinocarsen.

Abstract

As our understanding of tumorigenesis increases, interference with the various signaling pathways of tumor cells has become an attractive approach to arresting tumor cell growth and overcoming chemoresistance. Among many intracellular signaling proteins, protein kinase C (PKC) isoenzymes have been identified as possible targets to render tumor cells more susceptible to apoptosis and growth arrest. We review the known biology of the alpha-isoenzyme of PKC in different cancers to provide a rational approach for developing targeted therapies using PKC modulators, including aprinocarsen, an antisense oligonucleotide (ASO) against PKC-alpha.

• Authors: A-R Hanauske, Karen Sundell, Michael Lahn
• Journal: Current pharmaceutical design (Curr Pharm Des) Vol. 10 Issue 16 Pg. 1923-36 ( 2004) ISSN: 1381-6128 [Print] United Arab Emirates
• PMID: 15180529 (Publication Type: Journal Article, Review)

Chemical References

• Enzyme Inhibitors
• Oligodeoxyribonucleotides, Antisense
• Thionucleotides
• ISIS 3521
• PRKCA protein, human
• Protein Kinase C
• Protein Kinase C-alpha

Topics

• Animals
• Enzyme Inhibitors (pharmacology, therapeutic use)
• Humans
• Neoplasms (drug therapy, enzymology)
• Oligodeoxyribonucleotides, Antisense (pharmacology, therapeutic use)
• Protein Kinase C (antagonists & inhibitors, physiology)
• Protein Kinase C-alpha
• Thionucleotides (pharmacology, therapeutic use)