Abstract
Identification of the key roles of protein kinases in signaling pathways leading to development of cancer has caused pharmacological interest to concentrate extensively on targeted therapies as a more specific and effective way for blockade of cancer progression. This review will mainly focus on inhibitors targeting these key components of cellular signaling by employing a technology-based point of view with respect to ATP- and non-ATP-competitive small molecule inhibitors and monoclonal antibodies of selected protein kinases, particularly, mammalian target of rapamycin (mTOR), BCR-ABL, MEK, p38 MAPK, EGFR PDGFR, VEGFR, HER2 and Raf. Inhibitors of the heat shock protein Hsp90 are also included in a separate section, as this protein plays an essential role for the maturation/proper activation of cancer-related protein kinases. In the following review, the molecular details of the mode of action of these inhibitors as well as the emergence of drug resistance encountered in several cases are discussed in light of the structural, molecular and clinical studies conducted so far.
Keywords: Rapamycin, ATP-Competitive Inhibitors, BCR-ABL variants, Imatinib, gastrointestinal stromal tumors (GIST), monoclonal antibodies
Current Cancer Drug Targets
Title: Protein Kinases as Drug Targets in Cancer
Volume: 6 Issue: 7
Author(s): Mehmet Alper Arslan, Ozgur Kutuk and Huveyda Basaga
Affiliation:
Keywords: Rapamycin, ATP-Competitive Inhibitors, BCR-ABL variants, Imatinib, gastrointestinal stromal tumors (GIST), monoclonal antibodies
Abstract: Identification of the key roles of protein kinases in signaling pathways leading to development of cancer has caused pharmacological interest to concentrate extensively on targeted therapies as a more specific and effective way for blockade of cancer progression. This review will mainly focus on inhibitors targeting these key components of cellular signaling by employing a technology-based point of view with respect to ATP- and non-ATP-competitive small molecule inhibitors and monoclonal antibodies of selected protein kinases, particularly, mammalian target of rapamycin (mTOR), BCR-ABL, MEK, p38 MAPK, EGFR PDGFR, VEGFR, HER2 and Raf. Inhibitors of the heat shock protein Hsp90 are also included in a separate section, as this protein plays an essential role for the maturation/proper activation of cancer-related protein kinases. In the following review, the molecular details of the mode of action of these inhibitors as well as the emergence of drug resistance encountered in several cases are discussed in light of the structural, molecular and clinical studies conducted so far.
Export Options
About this article
Cite this article as:
Arslan Mehmet Alper, Kutuk Ozgur and Basaga Huveyda, Protein Kinases as Drug Targets in Cancer, Current Cancer Drug Targets 2006; 6 (7) . https://dx.doi.org/10.2174/156800906778742479
DOI https://dx.doi.org/10.2174/156800906778742479 |
Print ISSN 1568-0096 |
Publisher Name Bentham Science Publisher |
Online ISSN 1873-5576 |
Call for Papers in Thematic Issues
Advances in Cancer Biomarkers and Potential Drug Targets: From Diagnosis to Therapy
Cancer biomarkers play a crucial role in the diagnosis, prognosis, and treatment of cancer. They provide valuable information for cancer detection, risk assessment, treatment selection, and monitoring response to therapy. With advancements in molecular biology and high-throughput technologies, there has been an increasing interest in identifying and characterizing cancer biomarkers ...read more
Novel Therapeutic Approaches to Target Drug Resistant Tumors
With the development of disciplines such as chemical biology and molecular biology, the genes or proteins closely related to tumor occurrence and development have gradually become clear. Targeted therapies targeting these genes or proteins provide more effective methods for tumor treatment. Tumor targeted drugs generally only act on specific targets ...read more
ROLE OF IMMUNE AND GENOTOXIC RESPONSE BIOMARKERS IN TUMOR MICROENVIRONMENT IN CANCER DIAGNOSIS AND TREATMENT
Biological biomarkers have been used in medical research as an indicator of a normal or abnormal process inside the body, or of a disease. Nowadays, various researchers are in process to explore and investigate the biological markers for the early assessment of cancer. DNA Damage response (DDR) pathways and immune ...read more
Targeting the battlefield between host and tumor: basic research and clinical practice on reshaping tumor immune microenvironment
Immune system protects host against malignant tumors through effector cells and molecules. Cancer development and its response to therapy are regulated by inflammation, which either promotes or suppresses cancer progression. Chronic inflammation facilitates cancer progression and treatment resistance, whereas induction of acute inflammatory reactions often lead to anti-cancer immune responses. ...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
-
MicroRNAs-based Therapy: A Novel and Promising Strategy for Cancer Treatment
MicroRNA Ethical Implications of Pharmacogenetics: Shaping the Future of the Field
Current Pharmacogenomics Intestinal MicrobiOMICS to Define Health and Disease in Human and Mice
Current Pharmaceutical Biotechnology The miRNAs and Epithelial-Mesenchymal Transition in Cancers
Current Pharmaceutical Design Interventions Against Sarcopenia in Older Persons
Current Pharmaceutical Design Host Pharmacogenetics in the Treatment of HIV and Cancer
Current Drug Safety Cancer Chemoprevention by Targeting the Epigenome
Current Drug Targets NFAT Gene Family in Inflammation and Cancer
Current Molecular Medicine A Potential Anticancer Agent 1,2-di(quinazolin-4-yl)diselane
Letters in Drug Design & Discovery DNA Repair and Resistance to Topoisomerase I Inhibitors: Mechanisms, Biomarkers and Therapeutic Targets
Current Medicinal Chemistry Potential Cardio-Protective Agents: A Resveratrol Review (2000-2019)
Current Pharmaceutical Design Commonalities and Differences Between Crohns Disease and Ulcerative Colitis: The Genetic Clues to their Interpretation
Inflammation & Allergy - Drug Targets (Discontinued) Editorial (Thematic Issue: Vaccines)
Recent Patents on Inflammation & Allergy Drug Discovery Perinatal Gene Transfer to the Liver
Current Pharmaceutical Design Rheumatoid Arthritis: Notable Biomarkers Linking to Chronic Systemic Conditions and Cancer
Current Pharmaceutical Design Docking Prediction for Luteolin Inhibiting TNF-α and NF-κB Pathway
Letters in Drug Design & Discovery Varlitinib Mediates Its Activity Through Down Regulating MAPK/EGFR Pathway in Oral Cancer
Current Proteomics Therapeutic Potential of Targeting Glypican-3 in Hepatocellular Carcinoma
Anti-Cancer Agents in Medicinal Chemistry Chemoprotective Mechanism of the Natural Compounds, Epigallocatechin- 3-O-Gallate, Quercetin and Curcumin Against Cancer and Cardiovascular Diseases
Current Medicinal Chemistry Liposomes as Anticancer Therapeutic Drug Carrier’s Systems: More than a Tour de Force
Current Nanomedicine