Abstract
PHA-E is a natural product extracted from red kidney beans, and it has been reported to induce cell apoptosis by blocking EGFR in lung cancer cells. Because EGF is the major in vivo competitor to PHA-E in clinical application, PHA-E must be proved that has better affinity to EGFR than EGF. This study would focus on how PHA-E tightly bind to EGFR and the results would compare with EGF. The adhesion force, measured by AFM, between EGFR and PHA-E was 207.14±74.42 pN that was higher than EGF (183.65±86.93 pN). The equilibrium dissociation constant of PHA-E and EGF to EGFR was 2.410-9±1.410-9 and 7.310-8±2.710-8, respectively, that could evaluate binding affinity. The result showed that binding affinity of PHA-E to EGFR was one order higher than EGF to EGFR. In the results of flow cytometer and confocal microscope, we found binding efficiency of EGF to EGFR was decrease as the concentration of PHA-E increased. In the analysis of Western blot, treatment of A-549 cells with PHA-E resulted in a dose-dependent decrease in EGFR phosphorylation. In conclusion, we found that PHA-E had better adhesion force and binding affinity to EGFR than that of the EGF. The interaction between PHA-E and EGFR could block EGF binding and then inhibit EGFR phosphorylation. PHA-E could be developed into a new target molecule for lung cancer treatment that could be immobilized on the drug carrier to guide therapeutic particles to the tumor site.
Keywords: Adhesion force, binding affinity, epidermal growth factor receptor, lung cancer, natural product, phytohemagglutinin erythroagglutinating, target molecule.
Current Medicinal Chemistry
Title:Evaluation of Adhesion Force and Binding Affinity of Phytohemagglutinin Erythroagglutinating to EGF Receptor on Human Lung Cancer Cells
Volume: 20 Issue: 19
Author(s): W.-T. Kuo, G.-C. Dong, C.-H. Yao, J.-Y. Huang and F.-H. Lin
Affiliation:
Keywords: Adhesion force, binding affinity, epidermal growth factor receptor, lung cancer, natural product, phytohemagglutinin erythroagglutinating, target molecule.
Abstract: PHA-E is a natural product extracted from red kidney beans, and it has been reported to induce cell apoptosis by blocking EGFR in lung cancer cells. Because EGF is the major in vivo competitor to PHA-E in clinical application, PHA-E must be proved that has better affinity to EGFR than EGF. This study would focus on how PHA-E tightly bind to EGFR and the results would compare with EGF. The adhesion force, measured by AFM, between EGFR and PHA-E was 207.14±74.42 pN that was higher than EGF (183.65±86.93 pN). The equilibrium dissociation constant of PHA-E and EGF to EGFR was 2.410-9±1.410-9 and 7.310-8±2.710-8, respectively, that could evaluate binding affinity. The result showed that binding affinity of PHA-E to EGFR was one order higher than EGF to EGFR. In the results of flow cytometer and confocal microscope, we found binding efficiency of EGF to EGFR was decrease as the concentration of PHA-E increased. In the analysis of Western blot, treatment of A-549 cells with PHA-E resulted in a dose-dependent decrease in EGFR phosphorylation. In conclusion, we found that PHA-E had better adhesion force and binding affinity to EGFR than that of the EGF. The interaction between PHA-E and EGFR could block EGF binding and then inhibit EGFR phosphorylation. PHA-E could be developed into a new target molecule for lung cancer treatment that could be immobilized on the drug carrier to guide therapeutic particles to the tumor site.
Export Options
About this article
Cite this article as:
Kuo W.-T., Dong G.-C., Yao C.-H., Huang J.-Y. and Lin F.-H., Evaluation of Adhesion Force and Binding Affinity of Phytohemagglutinin Erythroagglutinating to EGF Receptor on Human Lung Cancer Cells, Current Medicinal Chemistry 2013; 20 (19) . https://dx.doi.org/10.2174/0929867311320190007
DOI https://dx.doi.org/10.2174/0929867311320190007 |
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
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
Current advances in inherited cardiomyopathy
Describe in detail all novel advances in multimodality imaging related to inherited cardiomyopathy diagnosis and prognosis. Shed light to deeper phenotypic characterization. Acknowledge recent advances in genetics, genomics and precision medicineread 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
-
Non-Viral Delivery of RNA Interference Targeting Cancer Cells in Cancer Gene Therapy
Current Gene Therapy New Concepts for Glaucoma Implants - Controlled Aqueous Humor Drainage, Encapsulation Prevention and Local Drug Delivery
Current Pharmaceutical Biotechnology Fragment-Based Discovery of Inhibitors of Protein Kinase B
Current Topics in Medicinal Chemistry Systemic Therapies for Pancreatic Cancer - The Role of Pharmacogenetics
Current Drug Targets Retroviral Protein Transfer: Falling Apart to Make an Impact
Current Gene Therapy Hetero-Diels-Alder Reactions in the Synthesis of Biologically Active Nitrogen Compounds: A Review
Current Organic Synthesis Adrenergic Receptors as Targets for Cancer Treatment - A Perspective for Future Studies
Current Cancer Therapy Reviews Glycation Induced Generation of Amyloid Fibril Structures by Glucose Metabolites
Protein & Peptide Letters Synthesis, Characterization, and Molecular Structure of a Novel Zinc (II) Complex: Assessment of Impact of MDR1Pgp Expression on its Cytotoxic Activity
Medicinal Chemistry Editorial [ Hot topic: Pharmaceutical Design of Novel Anticancer Agents: A Lesson from Nature (Executive Editor: Q. Ping Dou)]
Current Pharmaceutical Design Space Radiation Dosimetry: Overview and Recent Developments
Recent Patents on Space Technology Improved Identification of Cytokines Using Feature Selection Techniques
Letters in Organic Chemistry Air Pollution, Platelet Activation and Atherosclerosis
Inflammation & Allergy - Drug Targets (Discontinued) Dexamethasone Reduces Cell Adhesion and Migration of T47D Breast Cancer Cell Line
Anti-Cancer Agents in Medicinal Chemistry Apoptosis Suppression by Candidate Oncogene PLAC8 is Reversed in Other Cell Types
Current Cancer Drug Targets Electrochemical Immunosensors Based on Nanostructured Materials for Sensing of Prostate-Specific Antigen: A Review
Current Medicinal Chemistry Signal Transducer and Activator of Transcription 3 Signaling Pathway: A Potential Target in Sarcoma Treatment
Current Enzyme Inhibition From Nanotechnology to Nanomedicine: Applications to Cancer Research
Current Molecular Medicine Inhibition of Pyruvate Dehydrogenase Kinase as a Therapeutic Strategy against Cancer
Current Topics in Medicinal Chemistry Potential Beneficial Effects of Garlic in Oncohematology
Mini-Reviews in Medicinal Chemistry