Classical PKC isoforms in cancer.
Protein kinases C (PKCs) are a family of serine/threonine kinases which are involved in tumor formation and progression. Although PKC over-expression has been shown to contribute to cell transformation, PKCs are not considered to be classical oncogenes which are activated by mutations, but considered as tumor promoters that enhance multiple cellular signaling pathways. Over the last two decades a lot of evidence has emerged demonstrating a role for various PKC isoforms in cancer. Small molecular weight inhibitors and antisense molecules have been developed, specifically targeting the calcium dependent classical isoforms of PKC. This review focuses on the role of classical PKCs in cancer and the results obtained by attempting to inhibit these enzymes to achieve a therapeutic benefit.
Martiny-Baron
Georg
G
Novartis Institutes for Biomedical Research, Expertise Platform Kinases, Klybeckstr. 142, CH 4002 Basel, Switzerland. georg.martiny-baron@novartis.com
Fabbro
Doriano
D
D000818:Animals; D000970:Antineoplastic Agents / Q000494:pharmacology* / Q000627:therapeutic use; D006801:Humans; D009369:Neoplasms / Q000188:drug therapy / Q000201:enzymology*; D009841:Oligonucleotides / Q000494:pharmacology / Q000627:therapeutic use; D011493:Protein Kinase C / Q000037:antagonists & inhibitors / Q000502:physiology*; D064546:Protein Kinase C beta; D051571:Protein Kinase C-alpha / Q000037:antagonists & inhibitors / Q000502:physiology; D047428:Protein Kinase Inhibitors / Q000494:pharmacology* / Q000627:therapeutic use; D015398:Signal Transduction
D000970:Antineoplastic Agents; D009841:Oligonucleotides; D047428:Protein Kinase Inhibitors; C087857:protein kinase C gamma; D011493:Protein Kinase C; D064546:Protein Kinase C beta; D051571:Protein Kinase C-alpha