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
-
Fluorescent SNAP-Tag Galectin Fusion Proteins as Novel Tools in Glycobiology
Current Pharmaceutical Design Overview of Current Practice and Future Trends in Thromboprophylaxis for General Surgery
Vascular Disease Prevention (Discontinued) Adrenergic Action in Breast Cancer
Current Cancer Therapy Reviews Dynamic Simulations of Pathways Downstream of ERBB-Family, Including Mutations and Treatments: Concordance with Experimental Results
Current Cancer Drug Targets Fundamental Concepts of the Angiogenic Process
Current Molecular Medicine Impact of High Protein Intake on Viral Load and Hematological Parameters in HIV-infected Patients
Current HIV Research Quercetin and MicroRNA Interplay in Apoptosis Regulation in Ovarian Cancer
Current Pharmaceutical Design Formulation, Optimization and <i>In vitro / In vivo</i> Characterization of Spray Dried Doxorubicin Loaded Folic Acid Conjugated Gelatin Nanoparticles
Current Molecular Pharmacology IL-17 and its Receptor Complex as Therapeutic Targets in Arthritis
Immunology, Endocrine & Metabolic Agents in Medicinal Chemistry (Discontinued) Preface
Current Pharmaceutical Design Targeting the G2/M Transition for Antitumor Therapy
Letters in Drug Design & Discovery Hypoxia-Inducible Factor: A Potential Therapeutic Target for Rheumatoid Arthritis
Current Drug Targets Natural Products Targeting Cancer Stem Cells: A Revisit
Current Medicinal Chemistry Naturally Occurring NF-κB Inhibitors
Mini-Reviews in Medicinal Chemistry Genomics of Chronic Obstructive Pulmonary Disease (COPD); Exploring the SNPs of Protease-Antiprotease Pathway
Current Genomics Modulation of Angiogenesis for Cancer Prevention: Strategies Based On Antioxidants and Copper Deficiency
Current Pharmaceutical Design A Classification Method for Microarrays Based on Diversity
Current Bioinformatics Application of Molecular Imaging Technologies in Antitumor Drug Development and Therapy
Current Pharmaceutical Design Discovery of Anticancer Agents from 2-Pyrazoline-Based Compounds
Current Medicinal Chemistry Syntheses and Biological Activities of triazole-based Sulfonamides
Current Organic Chemistry