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
-
Accelerated Partial Breast Irradiation- Pros and Cons
Reviews on Recent Clinical Trials A Review of Recent Patents on the ASICs as a Key Drug Target
Recent Patents on Biotechnology Patent Selections
Recent Patents on DNA & Gene Sequences 5-HT3 Receptors: A Potential Therapeutic Target for Epilepsy
Current Neuropharmacology ZD6474, a Small Molecule Tyrosine Kinase Inhibitor, Potentiates the Anti-Tumor and Anti-Metastasis Effects of Radiation for Human Nasopharyngeal Carcinoma
Current Cancer Drug Targets Proteinase-Activated Receptor-2: Physiological and Pathophysiological Roles
Current Medicinal Chemistry - Cardiovascular & Hematological Agents Current Challenges and Implications of Proteogenomic Approaches in Prostate Cancer
Current Topics in Medicinal Chemistry Targeting ADAM12 in Human Disease: Head, Body or Tail?
Current Pharmaceutical Design Necroptosis: Who Knew There were so Many Interesting Ways to Die?
CNS & Neurological Disorders - Drug Targets A Review on Clinical Management and Pharmacological Therapy on Hereditary Haemorrhagic Telangiectasia (HHT)
Current Vascular Pharmacology Vascular Disrupting Agents (VDA) in Oncology: Advancing Towards New Therapeutic Paradigms in the Clinic
Current Drug Targets Azo Reductase- Activated Colon- Targeting Prodrugs of Aminosalicylates for Inflammatory Bowel Disease: Preparation, Pharmacokinetic and Pharmacodynamic Profile
Inflammation & Allergy - Drug Targets (Discontinued) Immunotherapy: A Potential Approach to Targeting Cancer Stem Cells
Current Cancer Drug Targets Sex Differences in Alcohol Use Disorder
Current Medicinal Chemistry Telomere Maintenance Mechanisms in Cancer: Clinical Implications
Current Pharmaceutical Design Curcumin: A Dietary Phytochemical for Targeting the Phenotype and Function of Dendritic Cells
Current Medicinal Chemistry Development of Pin1 Inhibitors and their Potential as Therapeutic Agents
Current Medicinal Chemistry Progress in Evaluation of Pathologic Response to Neoadjuvant Chemotherapy of Breast Cancer
Anti-Cancer Agents in Medicinal Chemistry The Blood-Brain Barrier in Multiple Sclerosis: microRNAs as Key Regulators
CNS & Neurological Disorders - Drug Targets Progress of HDAC Inhibitor Panobinostat in the Treatment of Cancer
Current Drug Targets