Abstract
Over the last ten years, several new and therapeutically relevant cancer drugs targeting tyrosine kinase signaling pathways have been developed. Tyrosine kinase inhibitors (TKIs) are a pharmaceutical class of small molecules, orally available, well-tolerated, worldwide approved drugs for the treatment of several neoplasms, including lung, breast, kidney and pancreatic cancer as well as gastro-intestinal stromal tumors and chronic myeloid leukemia. This comprehensive review focuses on the most relevant members of the first and the second generation TKIs designed to interact with receptor and nonreceptor TKs. Attention is mainly focused on molecular mechanisms in in vitro and in vivo models related to the clinical activity of the drugs and to the development of resistance to treatment, still the major challenge in cancer research and care.
Keywords: Angiogenesis, HER family, multitarget, nonreceptors, receptors, resistance, tyrosine kinase inhibitors
Current Cancer Drug Targets
Title: Tyrosine Kinase Inhibitors
Volume: 10 Issue: 5
Author(s): C. Natoli, B. Perrucci, F. Perrotti, L. Falchi and S. Iacobelli
Affiliation:
Keywords: Angiogenesis, HER family, multitarget, nonreceptors, receptors, resistance, tyrosine kinase inhibitors
Abstract: Over the last ten years, several new and therapeutically relevant cancer drugs targeting tyrosine kinase signaling pathways have been developed. Tyrosine kinase inhibitors (TKIs) are a pharmaceutical class of small molecules, orally available, well-tolerated, worldwide approved drugs for the treatment of several neoplasms, including lung, breast, kidney and pancreatic cancer as well as gastro-intestinal stromal tumors and chronic myeloid leukemia. This comprehensive review focuses on the most relevant members of the first and the second generation TKIs designed to interact with receptor and nonreceptor TKs. Attention is mainly focused on molecular mechanisms in in vitro and in vivo models related to the clinical activity of the drugs and to the development of resistance to treatment, still the major challenge in cancer research and care.
Export Options
About this article
Cite this article as:
Natoli C., Perrucci B., Perrotti F., Falchi L. and Iacobelli S., Tyrosine Kinase Inhibitors, Current Cancer Drug Targets 2010; 10 (5) . https://dx.doi.org/10.2174/156800910791517208
DOI https://dx.doi.org/10.2174/156800910791517208 |
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
-
A novel NGR-conjugated peptide targets DNA damage responses for radiosensitization
Current Cancer Drug Targets Therapeutic Targeting of Cancers with Loss of PTEN Function
Current Drug Targets Rational Drug Design of G-Quartet DNA as Anti-Cancer Agents
Current Pharmaceutical Design Endothelial Progenitor Cells: Hope Beyond Controversy
Current Cancer Drug Targets Curcumin Suppresses Tumor Growth and Angiogenesis in Human Glioma Cells Through Modulation of Vascular Endothelial Growth Factor/ Angiopoietin-2/Thrombospondin-1 Signaling
CNS & Neurological Disorders - Drug Targets mTOR Inhibition and the Tumor Vasculature
Current Angiogenesis (Discontinued) Recent Patents on the Development of c-Met Kinase Inhibitors
Recent Patents on Anti-Cancer Drug Discovery Cyclophilin function in Cancer; lessons from virus replication
Current Molecular Pharmacology MtDNA As a Cancer Marker: A Finally Closed Chapter?
Current Genomics Herpesvirus Saimiri-Based Gene Delivery Vectors
Current Gene Therapy Amino Acid Transporter-Targeted Radiotracers for Molecular Imaging in Oncology
Current Medicinal Chemistry Pro-Oxidant Milieu Blunts Scissors: Insight into Tumor Progression, Drug Resistance, and Novel Druggable Targets
Current Pharmaceutical Design Targeting Mevalonate Pathway in Cancer Treatment: Repurposing of Statins
Recent Patents on Anti-Cancer Drug Discovery Part II: Targeted Particles for Imaging of Anticancer Immune Responses
Current Drug Delivery Patent Selections
Recent Patents on Biotechnology Role of Natural Plant Products Against Alzheimer’s Disease
CNS & Neurological Disorders - Drug Targets A Century of Thioxanthones: Through Synthesis and Biological Applications
Current Medicinal Chemistry Small Molecular Inhibitors Targeting Chromatin Regulating Proteins for Cancer
Current Protein & Peptide Science C-glycosyl Flavone from Urginea indica Inhibits Growth and Dissemination of Ehrlich Ascites Carcinoma Cells in Mice
Anti-Cancer Agents in Medicinal Chemistry Current Understanding of Epigenetics Driven Therapeutic Strategies in Colorectal Cancer Management
Endocrine, Metabolic & Immune Disorders - Drug Targets