Abstract
Epidermal Growth Factor Receptor (EGFR) is a transmembrane glycoprotein that constitutes one of the four members of ErbB family of tyrosine kinase receptors. Activation of EGFR leads to autophosphorylation of receptor tyrosine kinase that initiates a cascade of downstream signaling pathways involved in regulating cellular proliferation, differentiation, and survival. EGFR is abnormally activated by various mechanisms like receptor overexpression, mutation, ligand-dependent receptor dimerization, ligand-independent activation and is associated with the development of variety of human cancers. EGFR inhibition is one of the key targets for cancer chemotherapy. Approval of tyrosine kinase inhibitors such as erlotinib, gefitinib, and lapatinib for the treatment of non-small cell lung cancer led to tremendous development of novel EGFR inhibitors in the last decade. Diverse class of chemical compounds from the synthetic origin has been extensively studied. This review highlights the various classes of synthetically derived molecules which have been reported in the last few years as potential EGFR and EGFR/ErbB-2 dual inhibitors. A brief synthetic methodology to access these compounds has been highlighted along with the SAR. We strongly believe that this review will provide a platform to the synthetic chemists and biologists to design and synthesize new and potent compounds that inhibit EGFR and ErbB-2.
Keywords: Antibodies, Apoptosis, Carcinoma, EGFR, Heterocyclic, Proliferation.
Mini-Reviews in Medicinal Chemistry
Title:Review on EGFR Inhibitors: Critical Updates
Volume: 16 Issue: 14
Author(s): Davinder Singh, Bhupinder Kumar Attri, Rupinder Kaur Gill and Jitender Bariwal
Affiliation:
Keywords: Antibodies, Apoptosis, Carcinoma, EGFR, Heterocyclic, Proliferation.
Abstract: Epidermal Growth Factor Receptor (EGFR) is a transmembrane glycoprotein that constitutes one of the four members of ErbB family of tyrosine kinase receptors. Activation of EGFR leads to autophosphorylation of receptor tyrosine kinase that initiates a cascade of downstream signaling pathways involved in regulating cellular proliferation, differentiation, and survival. EGFR is abnormally activated by various mechanisms like receptor overexpression, mutation, ligand-dependent receptor dimerization, ligand-independent activation and is associated with the development of variety of human cancers. EGFR inhibition is one of the key targets for cancer chemotherapy. Approval of tyrosine kinase inhibitors such as erlotinib, gefitinib, and lapatinib for the treatment of non-small cell lung cancer led to tremendous development of novel EGFR inhibitors in the last decade. Diverse class of chemical compounds from the synthetic origin has been extensively studied. This review highlights the various classes of synthetically derived molecules which have been reported in the last few years as potential EGFR and EGFR/ErbB-2 dual inhibitors. A brief synthetic methodology to access these compounds has been highlighted along with the SAR. We strongly believe that this review will provide a platform to the synthetic chemists and biologists to design and synthesize new and potent compounds that inhibit EGFR and ErbB-2.
Export Options
About this article
Cite this article as:
Singh Davinder, Attri Kumar Bhupinder, Gill Kaur Rupinder and Bariwal Jitender, Review on EGFR Inhibitors: Critical Updates, Mini-Reviews in Medicinal Chemistry 2016; 16 (14) . https://dx.doi.org/10.2174/1389557516666160321114917
DOI https://dx.doi.org/10.2174/1389557516666160321114917 |
Print ISSN 1389-5575 |
Publisher Name Bentham Science Publisher |
Online ISSN 1875-5607 |
Call for Papers in Thematic Issues
Bioprospecting of Natural Products as Sources of New Multitarget Therapies
According to the Convention on Biological Diversity, bioprospecting is the exploration of biodiversity and indigenous knowledge to develop commercially valuable products for pharmaceutical and other applications. Bioprospecting involves searching for useful organic compounds in plants, fungi, marine organisms, and microorganisms. Natural products traditionally constituted the primary source of more than ...read more
Computational Frontiers in Medicinal Chemistry
The thematic issue "Computational Frontiers in Medicinal Chemistry" provides a robust platform for delving into state-of-the-art computational methodologies and technologies that significantly propel advancements in medicinal chemistry. This edition seeks to amalgamate top-tier reviews spotlighting the latest trends and breakthroughs in the fusion of computational approaches, including artificial intelligence (AI) ...read more
Mitochondria as a Therapeutic Target in Metabolic Disorders
Mitochondria are the primary site of adenosine triphosphate (ATP) production in mammalian cells. Moreover, these organelles are an important source of reactive oxygen and nitrogen species in virtually any nucleated cell type. The modulation of a myriad of cellular signaling pathways depends on the mitochondrial physiology. Mitochondrial dysfunction is observed ...read more
Natural Products and Dietary Supplements in Alleviation of Metabolic, Cardiovascular, and Neurological Disorders
Metabolic disorders like diabetes, obesity, inflammation, oxidative stress, cancer etc, cardiovascular disorders like angina, myocardial infarction, congestive heart failure etc as well as neurological disorders like Alzheimer?s, Parkinson?s, Epilepsy, Depression, etc are the global burden. They covered the major segment of the diseases and disorders from which the human community ...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
-
Endocrine and Antineoplastic Actions of Growth Hormone-Releasing Hormone Antagonists
Current Medicinal Chemistry Molecular Imaging of Apoptosis In Vivo with Scintigraphic and Optical Biomarkers – A Status Report
Anti-Cancer Agents in Medicinal Chemistry The Use of Innovative Tools to Reproduce Human Cancer Translocations: Lessons from the CRISPR/Cas System
Current Biotechnology Preface
Current Pharmaceutical Design The Roles of Vitamin D and Its Analogs in Inflammatory Diseases
Current Topics in Medicinal Chemistry Various Approaches for Medical Image Segmentation: A Survey
Current Medical Imaging Benzo[a]pyrene Toxicity and Inflammatory Disease
Current Rheumatology Reviews The Synthesis of Nano-Doxorubicin and its Anticancer Effect
Anti-Cancer Agents in Medicinal Chemistry Insulin-like Growth Factor: Current Concepts and New Developments in Cancer Therapy
Recent Patents on Anti-Cancer Drug Discovery Potential of Plant-Derived Natural Products in the Treatment of Leukemia and Lymphoma
Current Drug Targets Imaging of EGFR and EGFR Tyrosine Kinase Overexpression in Tumors by Nuclear Medicine Modalities
Current Pharmaceutical Design Synthesis, Photophysical and Photochemical Aspects of Phthalocyanines for Photodynamic Therapy
Current Organic Chemistry Targeting the Immune Niche within the Bone Marrow Microenvironment: The Rise of Immunotherapy in Multiple Myeloma
Current Cancer Drug Targets The Functions of F-box Proteins in Regulating the Epithelial to Mesenchymal Transition
Current Pharmaceutical Design Click Chemistry Based Functionalizations of Nucleoside, Nucleotide and Nucleic Acids
Current Organic Chemistry Synthesis, Molecular Docking and Biological Activity Evaluation of Alkoxy Substituted Chalcone Derivatives: Potential Apoptosis Inducing Agent on MCF-7 Cells
Anti-Cancer Agents in Medicinal Chemistry Bisphosphonates as Treatment of Bone Metastases
Current Pharmaceutical Design On The Edge of Validation – Cancer Protease Fibroblast Activation Protein
Mini-Reviews in Medicinal Chemistry Drug-Related Cardiotoxicity for the Treatment of Haematological Malignancies in Elderly
Current Pharmaceutical Design A Glimpse of Matrix Metalloproteinases in Diabetic Nephropathy
Current Medicinal Chemistry