Abstract
In the last years, PKC has become an attractive target for the treatment of cancer patients given its widely described role in carcinogenesis and tumor promotion. Despite the extensive research conducted on these phorbol ester receptors there is only limited knowledge about the contribution of each individual PKC isozyme in malignant transformation, mainly due to the different roles of each isozyme and their tissue-specificity. This diversity provides the unique opportunity to develop specific pharmacological agents, but the complex nature of the signaling pathways activated by different PKCs challenges selective drug therapies. Currently, several classes of PKC inhibitors including small molecule kinase inhibitors, biologic modulators, and anti-sense oligonucleotides are being evaluated for the treatment of different cancers where PKC isozymes were found to be deregulated as lung, colon, skin, prostate, and breast malignancies. In this article we will review which PKC isoforms are deregulated in different human cancers and summarize the mechanism of action of some of the major PKC modulators, analyzing the strengths and weaknesses of each one in the clinical setting.
Keywords: Cancer, clinical trials, PKC, tumor promotion, malignant transformation, specific pharmacological agents, anti-sense oligonucleotides, protein kinase C (PKC), therapeutic target, cell membrane receptors, several signaling cascades, cell cycle arrest, normal mammary cells, matrix metalloproteinases (MMP)
Current Pharmaceutical Biotechnology
Title: The Pros and Cons of Targeting Protein Kinase c (PKC) in the Management of Cancer Patients
Volume: 12 Issue: 11
Author(s): F. Coluccio Leskow, M. A. Krasnapolski and A. J. Urtreger
Affiliation:
Keywords: Cancer, clinical trials, PKC, tumor promotion, malignant transformation, specific pharmacological agents, anti-sense oligonucleotides, protein kinase C (PKC), therapeutic target, cell membrane receptors, several signaling cascades, cell cycle arrest, normal mammary cells, matrix metalloproteinases (MMP)
Abstract: In the last years, PKC has become an attractive target for the treatment of cancer patients given its widely described role in carcinogenesis and tumor promotion. Despite the extensive research conducted on these phorbol ester receptors there is only limited knowledge about the contribution of each individual PKC isozyme in malignant transformation, mainly due to the different roles of each isozyme and their tissue-specificity. This diversity provides the unique opportunity to develop specific pharmacological agents, but the complex nature of the signaling pathways activated by different PKCs challenges selective drug therapies. Currently, several classes of PKC inhibitors including small molecule kinase inhibitors, biologic modulators, and anti-sense oligonucleotides are being evaluated for the treatment of different cancers where PKC isozymes were found to be deregulated as lung, colon, skin, prostate, and breast malignancies. In this article we will review which PKC isoforms are deregulated in different human cancers and summarize the mechanism of action of some of the major PKC modulators, analyzing the strengths and weaknesses of each one in the clinical setting.
Export Options
About this article
Cite this article as:
Coluccio Leskow F., A. Krasnapolski M. and J. Urtreger A., The Pros and Cons of Targeting Protein Kinase c (PKC) in the Management of Cancer Patients, Current Pharmaceutical Biotechnology 2011; 12 (11) . https://dx.doi.org/10.2174/138920111798376950
DOI https://dx.doi.org/10.2174/138920111798376950 |
Print ISSN 1389-2010 |
Publisher Name Bentham Science Publisher |
Online ISSN 1873-4316 |
Call for Papers in Thematic Issues
Artificial Intelligence in Bioinformatics
Bioinformatics is an interdisciplinary field that analyzes and explores biological data. This field combines biology and information system. Artificial Intelligence (AI) has attracted great attention as it tries to replicate human intelligence. It has become common technology for analyzing and solving complex data and problems and encompasses sub-fields of machine ...read more
- Author Guidelines
- Graphical Abstracts
- Fabricating and Stating False Information
- Research Misconduct
- Post Publication Discussions and Corrections
- Publishing Ethics and Rectitude
- Increase Visibility of Your Article
- Archiving Policies
- Peer Review Workflow
- Order Your Article Before Print
- Promote Your Article
- Manuscript Transfer Facility
- Editorial Policies
- Allegations from Whistleblowers
Related Articles
-
Novel Histone Deacetylase Inhibitors for the Treatment of Pediatric Brain Tumors
Central Nervous System Agents in Medicinal Chemistry Cyclin-Dependent Kinase 4/6 (Cdk4/6) Inhibitors: Perspectives in Cancer Therapy and Imaging
Mini-Reviews in Medicinal Chemistry Seizures and Anticonvulsants in Brain Tumours: Frequency, Mechanisms and Anti-Epileptic Management
Current Pharmaceutical Design Fabrication of Poly Hydroxybutyrate-Polyethylene Glycol-Folic Acid Nanoparticles Loaded by Paclitaxel
Current Drug Delivery The Emerging Role of Metabotropic Glutamate Receptors in the Pathophysiology of Chronic Stress-Related Disorders
Current Neuropharmacology Second Generation Taxanes: from the Natural Framework to the Challenge of Drug Resistance
Current Medicinal Chemistry - Anti-Cancer Agents Potassium Channels: Novel Emerging Biomarkers and Targets for Therapy in Cancer
Recent Patents on Anti-Cancer Drug Discovery Meet Our Associate Editor
Current Bioactive Compounds ErbB Targeted Drugs and Angiogenesis
Current Vascular Pharmacology A Review of the ADAMTS Family, Pharmaceutical Targets of the Future
Current Pharmaceutical Design Natural and Engineered Cystine Knot Miniproteins for Diagnostic and Therapeutic Applications
Current Pharmaceutical Design Natural Products as Exquisitely Potent Cytotoxic Payloads for Antibody- Drug Conjugates
Current Topics in Medicinal Chemistry Targeted Ultrasound Imaging of Cancer: An Emerging Technology on its Way to Clinics
Current Pharmaceutical Design Apoptotic Signaling in Pancreatic Cancer – Therapeutic Application (Supplemental Data)
Current Cancer Therapy Reviews Safety of Multi-Targeted Kinase Inhibitors as Monotherapy Treatment of Cancer: A Systematic Review of the Literature
Current Drug Safety Recently Patented Applications of Homologous Cellular and Extracellular Agents as Therapeutics or Targets for the Prevention of Restenosis Post- Angioplasty
Recent Patents on Cardiovascular Drug Discovery Use of E. coli Purine Nucleoside Phosphorylase in the Treatment of Solid Tumors
Current Pharmaceutical Design MBD1 is an Epigenetic Regulator of KEAP1 in Pancreatic Cancer
Current Molecular Medicine The Ubiquitin-Proteasome System (UPS) and the Mechanism of Action of Bortezomib
Current Pharmaceutical Design Tumor Angiogenesis and VEGFR-2: Mechanism, Pathways and Current Biological Therapeutic Interventions
Current Drug Metabolism