Abstract
Although the role of serine/threonine protein kinase C (PKC) in malignant transformation is known from decades, an anti-PKC based approach in cancer therapy was hampered for the difficulties in developing pharmacological compounds able to selectively inhibit specific PKC isoforms. In this review, the role of PKC-η and PKC-δ in promoting and counteracting tumor progression in different types of cancer, respectively, will be discussed in relationship with promising therapeutic perspectives based either on small molecule inhibitors or on natural compounds. Among a miriad of molecules able to modulate PKC activity, we will focus on the role of the enzastaurin and briostatin-1, which already entered clinical trials for several human cancers.
Keywords: PKC, apoptosis, differentiation, tumorigenesis
Mini-Reviews in Medicinal Chemistry
Title: Perspectives of Protein Kinase C (PKC) Inhibitors as Anti-Cancer Agents
Volume: 9 Issue: 4
Author(s): A. Gonelli, C. Mischiati, R. Guerrini, R. Voltan, S. Salvadori and G. Zauli
Affiliation:
Keywords: PKC, apoptosis, differentiation, tumorigenesis
Abstract: Although the role of serine/threonine protein kinase C (PKC) in malignant transformation is known from decades, an anti-PKC based approach in cancer therapy was hampered for the difficulties in developing pharmacological compounds able to selectively inhibit specific PKC isoforms. In this review, the role of PKC-η and PKC-δ in promoting and counteracting tumor progression in different types of cancer, respectively, will be discussed in relationship with promising therapeutic perspectives based either on small molecule inhibitors or on natural compounds. Among a miriad of molecules able to modulate PKC activity, we will focus on the role of the enzastaurin and briostatin-1, which already entered clinical trials for several human cancers.
Export Options
About this article
Cite this article as:
Gonelli A., Mischiati C., Guerrini R., Voltan R., Salvadori S. and Zauli G., Perspectives of Protein Kinase C (PKC) Inhibitors as Anti-Cancer Agents, Mini-Reviews in Medicinal Chemistry 2009; 9 (4) . https://dx.doi.org/10.2174/138955709787847967
DOI https://dx.doi.org/10.2174/138955709787847967 |
Print ISSN 1389-5575 |
Publisher Name Bentham Science Publisher |
Online ISSN 1875-5607 |
Call for Papers in Thematic Issues
Bioprospecting of Natural Products as Sources of New Multitarget Therapies
According to the Convention on Biological Diversity, bioprospecting is the exploration of biodiversity and indigenous knowledge to develop commercially valuable products for pharmaceutical and other applications. Bioprospecting involves searching for useful organic compounds in plants, fungi, marine organisms, and microorganisms. Natural products traditionally constituted the primary source of more than ...read more
Computational Frontiers in Medicinal Chemistry
The thematic issue "Computational Frontiers in Medicinal Chemistry" provides a robust platform for delving into state-of-the-art computational methodologies and technologies that significantly propel advancements in medicinal chemistry. This edition seeks to amalgamate top-tier reviews spotlighting the latest trends and breakthroughs in the fusion of computational approaches, including artificial intelligence (AI) ...read more
Mitochondria as a Therapeutic Target in Metabolic Disorders
Mitochondria are the primary site of adenosine triphosphate (ATP) production in mammalian cells. Moreover, these organelles are an important source of reactive oxygen and nitrogen species in virtually any nucleated cell type. The modulation of a myriad of cellular signaling pathways depends on the mitochondrial physiology. Mitochondrial dysfunction is observed ...read more
Natural Products and Dietary Supplements in Alleviation of Metabolic, Cardiovascular, and Neurological Disorders
Metabolic disorders like diabetes, obesity, inflammation, oxidative stress, cancer etc, cardiovascular disorders like angina, myocardial infarction, congestive heart failure etc as well as neurological disorders like Alzheimer?s, Parkinson?s, Epilepsy, Depression, etc are the global burden. They covered the major segment of the diseases and disorders from which the human community ...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
-
Current and Emerging Therapies in Primary Myelofibrosis
Cardiovascular & Hematological Disorders-Drug Targets Stereoselective Pharmacodynamics and Pharmacokinetics of Proton Pump Inhibitors
Current Drug Metabolism Targeting Epidermal Growth Factor Receptor in Solid Tumors: Critical Evaluation of the Biological Importance of Therapeutic Monoclonal Antibodies
Current Medicinal Chemistry Genetic and Epigenetic Studies for Determining Molecular Targets of Natural Product Anticancer Agents
Current Cancer Drug Targets Combination of Free Software, Light Microscopy and Non-specific Dyes for a High-throughput Analysis in Live/Dead Cell Count
Current Pharmaceutical Analysis PET Imaging to Monitor Cancer Therapy
Current Pharmaceutical Biotechnology Emerging Roles of MicroRNA-22 in Human Disease and Normal Physiology
Current Molecular Medicine Meet the Associate Editorial Board Member
Recent Patents on Anti-Cancer Drug Discovery Resveratrol in Medicinal Chemistry: A Critical Review of its Pharmacokinetics, Drug-Delivery, and Membrane Interactions
Current Medicinal Chemistry CDK Inhibitors: From the Bench to Clinical Trials
Current Drug Targets Prophylactic Potential of Conventional and Supercritical Garlic Extracts to Alleviate Diet Related Malfunctions
Recent Patents on Food, Nutrition & Agriculture Pharmacokinetics of Polymeric Micelles for Cancer Treatment
Current Drug Metabolism DNA Instability at Chromosomal Fragile Sites in Cancer
Current Genomics Lithium - Pharmacological and Toxicological Aspects: The Current State of the Art
Current Medicinal Chemistry Functions of Polo-Like Kinases: A Journey From Yeast To Humans
Protein & Peptide Letters Transmembrane Phosphatases and Cancer Development, the Role of Protein Tyrosine Phosphatase-kappa (PTPκ) and Protein Tyrosine Phosphatase-mu (PTPμ)
Current Signal Transduction Therapy Circumventing Immune Tolerance Through Epigenetic Modification
Current Pharmaceutical Design Applications of Artificial Neural Networks in Medical Science
Current Clinical Pharmacology Transbronchial Needle Aspiration (TBNA): Past Present and Future
Current Respiratory Medicine Reviews The Role of Target Therapy in the Treatment of Gastrointestinal Noncolorectal Cancers: Clinical Impact and Cost Consideration
Current Cancer Drug Targets