Abstract
Dysregulation of receptor tyrosine kinases (RTKs) in cancer cells is extremely common. Overexpression of human epidermal growth factor receptor (EGFR/HER) tyrosine kinase is correlated with tumor aetiology, progression and poor prognosis. Their activation is also observed frequently in human cancers. Therefore, RTKs have been identified as important therapeutic targets in oncology. Many therapeutic methods have been developed based on inhibition of EGFR and HER-2. Herein, we will discuss recent progress in the development of EGFR/HER-2 tyrosine kinase inhibitors. We will focus on the design strategies, pharmacological profiles and structure-activity relationships (SARs) of EGFR and HER-2 inhibitors.
Keywords: EGFR, ERBB, HER-2, structure-activity relationship, tyrosine kinase.
Current Medicinal Chemistry
Title:Insight into the Medicinal Chemistry of EGFR and HER-2 Inhibitors
Volume: 21 Issue: 11
Author(s): C. Wang, H. Gao, J. Dong, F. Wang, P. Li and J. Zhang
Affiliation:
Keywords: EGFR, ERBB, HER-2, structure-activity relationship, tyrosine kinase.
Abstract: Dysregulation of receptor tyrosine kinases (RTKs) in cancer cells is extremely common. Overexpression of human epidermal growth factor receptor (EGFR/HER) tyrosine kinase is correlated with tumor aetiology, progression and poor prognosis. Their activation is also observed frequently in human cancers. Therefore, RTKs have been identified as important therapeutic targets in oncology. Many therapeutic methods have been developed based on inhibition of EGFR and HER-2. Herein, we will discuss recent progress in the development of EGFR/HER-2 tyrosine kinase inhibitors. We will focus on the design strategies, pharmacological profiles and structure-activity relationships (SARs) of EGFR and HER-2 inhibitors.
Export Options
About this article
Cite this article as:
Wang C., Gao H., Dong J., Wang F., Li P. and Zhang J., Insight into the Medicinal Chemistry of EGFR and HER-2 Inhibitors, Current Medicinal Chemistry 2014; 21 (11) . https://dx.doi.org/10.2174/0929867320666131119124646
DOI https://dx.doi.org/10.2174/0929867320666131119124646 |
Print ISSN 0929-8673 |
Publisher Name Bentham Science Publisher |
Online ISSN 1875-533X |
Call for Papers in Thematic Issues
Advances in Medicinal Chemistry: From Cancer to Chronic Diseases.
The broad spectrum of the issue will provide a comprehensive overview of emerging trends, novel therapeutic interventions, and translational insights that impact modern medicine. The primary focus will be diseases of global concern, including cancer, chronic pain, metabolic disorders, and autoimmune conditions, providing a broad overview of the advancements in ...read more
Approaches to the treatment of chronic inflammation
Chronic inflammation is a hallmark of numerous diseases, significantly impacting global health. Although chronic inflammation is a hot topic, not much has been written about approaches to its treatment. This thematic issue aims to showcase the latest advancements in chronic inflammation treatment and foster discussion on future directions in this ...read more
Cellular and Molecular Mechanisms of Non-Infectious Inflammatory Diseases: Focus on Clinical Implications
The Special Issue covers the results of the studies on cellular and molecular mechanisms of non-infectious inflammatory diseases, in particular, autoimmune rheumatic diseases, atherosclerotic cardiovascular disease and other age-related disorders such as type II diabetes, cancer, neurodegenerative disorders, etc. Review and research articles as well as methodology papers that summarize ...read more
Chalcogen-modified nucleic acid analogues
Chalcogen-modified nucleosides, nucleotides and oligonucleotides have been of great interest to scientific research for many years. The replacement of oxygen in the nucleobase, sugar or phosphate backbone by chalcogen atoms (sulfur, selenium, tellurium) gives these biomolecules unique properties resulting from their altered physical and chemical properties. The continuing interest in ...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
- Announcements
Related Articles
-
L-Arginine Modulates Glucose and Lipid Metabolism in Obesity and Diabetes
Current Protein & Peptide Science Polymer Coated Iron Nanoparticles: Radiolabeling & In vitro Studies
Current Radiopharmaceuticals Lymphatics and Inflammation
Current Medicinal Chemistry Single-Photon Emission Computed Tomography Tracers for Predicting and Monitoring Cancer Therapy
Current Pharmaceutical Biotechnology Therapeutic Rationale for mTOR Inhibition in Advanced Renal Cell Carcinoma
Current Clinical Pharmacology Functional Foods: Salient Features and Clinical Applications
Current Drug Targets - Immune, Endocrine & Metabolic Disorders Central Nervous System Vasculitis: Still More Questions than Answers
Current Neuropharmacology The Role of IRF1 and IRF2 Transcription Factors in Leukaemogenesis
Current Gene Therapy Stilbenes and Xanthones from Medicinal Plants as Potential Antitumor Agents
Current Bioactive Compounds Trichothecin from Endophytic Fungus Trichothecium sp. and its Anticancer Effect on Murine Melanoma and Breast Cancer Cell Lines
Current Biochemical Engineering (Discontinued) Neuregulin Signaling in Pieces-Evolution of the Gene Family
Current Pharmaceutical Design Phytochemical and Pharmacological Insight on Sesamol: An Updated Review
Current Bioactive Compounds Psychological Sequelae of Ovarian Cancer Screening and Genetic Testing for Ovarian Cancer Susceptibility
Current Women`s Health Reviews Depression, Serotonin and Tryptophan
Current Pharmaceutical Design Predictive Efficacy Biomarkers of Programmed Cell Death 1/Programmed Cell Death 1 Ligand Blockade Therapy
Recent Patents on Anti-Cancer Drug Discovery 3,4-Dihydropyrimidin-2(1H)-one C5 Amides as Inhibitors of T NFα Production: Synthesis, Biological Evaluation and Molecular Modeling
Letters in Drug Design & Discovery PI3K/Akt/mTOR Pathway Inhibitors in Cancer: A Perspective on Clinical Progress
Current Medicinal Chemistry Graphical Abstracts
Letters in Drug Design & Discovery Design and Synthesis of Novel Thioethers Derived from 1,5-Diphenyl-6- thioxo-6,7-dihydro-1H-pyrazolo[3,4-d]pyrimidin-4(5H)-ones as Antiangiogenic Agents
Letters in Drug Design & Discovery Determination of Epsilon Aminocaproic Acid Based on Charge Transfer Complexation with p-Nitrophenlol by Spectrophotometry
Current Pharmaceutical Analysis