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
-
Recent Advances in Thymidine Kinase 2 (TK2) Inhibitors and New Perspectives for Potential Applications
Current Pharmaceutical Design PPARs in Diseases: Control Mechanisms of Inflammation
Current Medicinal Chemistry Long Term Cardiovascular Risk in Women
Vascular Disease Prevention (Discontinued) Activation of Intrinsic Apoptosis and G1 Cell Cycle Arrest by a Triazole Precursor, N-(4-chlorophenyl)-2-(4-(3,4,5-trimethoxybenzyloxy)benzoyl)-hydrazinecarbothioamide in Breast Cancer Cell Line
Anti-Cancer Agents in Medicinal Chemistry Synthesis of Novel 2,3,4-trisubstituted-oxazolidine Derivatives and In Vitro Cytotoxic Evaluation
Medicinal Chemistry Tissue Distribution and Pharmacodynamics: A Complicated Relationship
Current Drug Metabolism Biodiversity and Chemodiversity: Future Perspectives in Bioprospecting
Current Drug Targets Screening Novel SAHA Derivatives as Anti-lung Carcinoma Agents: Synthesis, Biological Evaluation, Docking Studies and Further Mechanism Research between Apoptosis and Autophagyetween Apoptosis and Autophagy
Anti-Cancer Agents in Medicinal Chemistry Novel Patents and Cancer Therapies for Transforming Growth Factor- Beta and Urokinase Type Plasminogen Activator: Potential Use of Their Interplay in Tumorigenesis
Recent Patents on Anti-Cancer Drug Discovery Anti-angiogenic Treatment in Metastatic Colorectal Cancer: Current Issues and Future Aims
Current Cancer Therapy Reviews Cell Cycle Regulatory Kinase Modulators: Interim Progress and Issues
Current Topics in Medicinal Chemistry Monoclonal Antibodies as a Tool for Structure-Function Studies of the MDR1-P-Glycoprotein
Current Protein & Peptide Science The Microarray Gene Profiling Analysis of Glioblastoma Cancer Cells Reveals Genes Affected by FAK Inhibitor Y15 and Combination of Y15 and Temozolomide
Anti-Cancer Agents in Medicinal Chemistry Pooled RNAi Screens - Technical and Biological Aspects
Current Genomics CEACAM1 in Malignant Melanoma: A Diagnostic and Therapeutic Target
Current Topics in Medicinal Chemistry Focal Adhesion Kinase as a Cancer Therapy Target
Anti-Cancer Agents in Medicinal Chemistry Extracellular Vesicles: A New Nano Tool for the Treatment of Inflammatory Bowel Diseases
Current Nanoscience Box-Behnken Design Optimized TPGS Coated Bovine Serum Albumin Nanoparticles Loaded with Anastrozole
Current Drug Delivery The Role of Mass Spectrometry in the “Omics” Era
Current Organic Chemistry Glucocorticoid Receptor Interacting Co-regulators: Putative Candidates for Future Drug Targeting Therapy
Mini-Reviews in Medicinal Chemistry