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
Chemistry of Materials and Emerging Techniques: Future of Drug Discovery and Medicinal Product Developments
In drug discovery, established knowledge of functional groups, their chemical behaviors, and structure-activity relationships favor chemists to achieve desired efficacy and safety profiles within the novel designed medicinal products. Here, judicious integration of different tools and techniques of chemistry also plays a fundamental role towards the selection of the processes ...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
Drugs and Mitochondria
Mitochondria play a central role in the life and death of cells. They are not merely the center for energy metabolism but are also the headquarters for different catabolic and anabolic processes, calcium fluxes, and various signaling pathways. Mitochondria maintain homeostasis in the cell by interacting with reactive oxygen-nitrogen species ...read more

- Author Guidelines
- Bentham Author Support Services (BASS)
- 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
-
Recent Advances in Minimal Access Surgery for Infants and Children
Current Pediatric Reviews Inappropriate Use of Proton Pump Inhibitor Among Elderly Patients in British Columbia: What are the Long-term Adverse Events?
Current Drug Safety Enrichment of Up-regulated and Down-regulated Gene Clusters Using Gene Ontology, miRNAs and lncRNAs in Colorectal Cancer
Combinatorial Chemistry & High Throughput Screening Nitrogen-Containing Heterocycles as Anticancer Agents: An Overview
Anti-Cancer Agents in Medicinal Chemistry The Tumor Stroma as Mediator of Drug Resistance - A Potential Target to Improve Cancer Therapy?
Current Pharmaceutical Biotechnology Mitochondrial DNA Mutations in Cancer: A Review
Current Topics in Medicinal Chemistry Prophylactic Potential of Conventional and Supercritical Garlic Extracts to Alleviate Diet Related Malfunctions
Recent Patents on Food, Nutrition & Agriculture Silencing GPX3 Expression Promotes Tumor Metastasis in Human Thyroid Cancer
Current Protein & Peptide Science Systemic Sclerosis: Clinical Manifestations
Current Rheumatology Reviews Application of Nanoparticles for Efficient Delivery of Quercetin in Cancer Cells
Current Medicinal Chemistry Targeting Cancer Stem Cells with Repurposed Drugs to Improve Current Therapies
Recent Patents on Anti-Cancer Drug Discovery Photodynamic Therapy using Carbohydrate Conjugated Porphyrins
Drug Design Reviews - Online (Discontinued) Molecular Pathways of Interferon-Stimulated Gene 15: Implications in Cancer
Current Protein & Peptide Science Therapeutic Implications of mTOR Inhibitors in the Treatment of Gastric Cancer
Current Cancer Drug Targets Impact of Oncogenic Protein Tyrosine Phosphatases in Cancer
Anti-Cancer Agents in Medicinal Chemistry Cancer Imaging Agents for Positron Emission Tomography: Beyond FDG
Current Medical Imaging An Integrative “Omics” Approach, for Identification of Bona Fides PLK1 Associated Biomarker in Esophageal Adenocarcinoma
Current Cancer Drug Targets Performance of the Iterative OSEM and HYPER Algorithm for Total-body PET at SUVmax with a Low 18F-FDG Activity, a Short Acquisition Time and Small Lesions
Current Medical Imaging Analysis of Comparative Proteomic and Potent Targets of Peniciketal A in Human Acute Monocytic Leukemia
Anti-Cancer Agents in Medicinal Chemistry Cadherins: The Superfamily Critically Involved in Breast Cancer
Current Pharmaceutical Design