Abstract
HER2 receptor, for its involvement in tumorigenesis, has been largely studied as topic in cancer research. In particular, the employment of trastuzumab (Herceptin), a humanized anti-HER2 antibody, showed several clinical benefits in the therapy against the breast cancer. Moreover, for its accessible extracellular domain, this receptor is considered an ideal target to deliver anticancer drugs for the receptormediated anticancer therapy. By now, monoclonal antibody and its fragments, affibody, and some peptides have been employed as targeting agents in order to deliver various drugs to HER2 positive tumor cells. In particular, the ability to perform a fast and reliable screening of a large number of peptide molecules would make possible the selection of highly specific compounds to the receptor target. In this regard, the availability of preparing a simplified synthetic model which is a good mimetic of the receptor target and can be used in a reliable screening method of ligands would be of a strategic importance for the development of selective HER2-targeting peptide molecules. Herein, we illustrate the importance of HER2-targeted anticancer therapies. We also report on a synthetic and effective mimetic of the receptor, which revealed to be a useful tool for the selection of specific HER2 ligands.
Keywords: Drug delivery systems, HER2 receptor, Screening methods, Selective ligand, Synthetic receptor fragment, Targeted cancer therapy.
Current Medicinal Chemistry
Title:HER2-Mediated Anticancer Drug Delivery: Strategies to Prepare Targeting Ligands Highly Specific for the Receptor
Volume: 22 Issue: 21
Author(s): Enrica Calce, Luca Monfregola, Michele Saviano and Stefania De Luca
Affiliation:
Keywords: Drug delivery systems, HER2 receptor, Screening methods, Selective ligand, Synthetic receptor fragment, Targeted cancer therapy.
Abstract: HER2 receptor, for its involvement in tumorigenesis, has been largely studied as topic in cancer research. In particular, the employment of trastuzumab (Herceptin), a humanized anti-HER2 antibody, showed several clinical benefits in the therapy against the breast cancer. Moreover, for its accessible extracellular domain, this receptor is considered an ideal target to deliver anticancer drugs for the receptormediated anticancer therapy. By now, monoclonal antibody and its fragments, affibody, and some peptides have been employed as targeting agents in order to deliver various drugs to HER2 positive tumor cells. In particular, the ability to perform a fast and reliable screening of a large number of peptide molecules would make possible the selection of highly specific compounds to the receptor target. In this regard, the availability of preparing a simplified synthetic model which is a good mimetic of the receptor target and can be used in a reliable screening method of ligands would be of a strategic importance for the development of selective HER2-targeting peptide molecules. Herein, we illustrate the importance of HER2-targeted anticancer therapies. We also report on a synthetic and effective mimetic of the receptor, which revealed to be a useful tool for the selection of specific HER2 ligands.
Export Options
About this article
Cite this article as:
Calce Enrica, Monfregola Luca, Saviano Michele and Luca De Stefania, HER2-Mediated Anticancer Drug Delivery: Strategies to Prepare Targeting Ligands Highly Specific for the Receptor, Current Medicinal Chemistry 2015; 22 (21) . https://dx.doi.org/10.2174/0929867322666150521091103
DOI https://dx.doi.org/10.2174/0929867322666150521091103 |
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
-
PGD and Prenatal Diagnosis: Comparison and Review in Different Genetic Disorders
Current Women`s Health Reviews The Cyclin-Dependent Kinase Inhibitor p21CDKN1A as a Target of Anti-Cancer Drugs
Current Cancer Drug Targets IgG4-Related Disease (IgG4+MOLPS) – Diagnostic Criteria and Diagnostic Problems
Current Immunology Reviews (Discontinued) Therapeutic Targeting of NLRP3 Inflammasomes by Natural Products and Pharmaceuticals: A Novel Mechanistic Approach for Inflammatory Diseases
Current Medicinal Chemistry Role of Resveratrol in Modulating microRNAs in Human Diseases: From Cancer to Inflammatory Disorder
Current Medicinal Chemistry Vasopressin and Related Peptides; Potential Value in Diagnosis, Prognosis and Treatment of Clinical Disorders
Current Drug Metabolism TRAIL Gene Therapy: From Preclinical Development to Clinical Application
Current Gene Therapy Protein Geranylgeranyltransferase Type 1 as a Target in Cancer
Current Cancer Drug Targets Patent Selections
Recent Patents on DNA & Gene Sequences Nanomedicine and its Application in Treatment of Microglia-mediated Neuroinflammation
Current Medicinal Chemistry Uncovering New Pharmacological Targets to Treat Neuropathic Pain by Understanding How the Organism Reacts to Nerve Injury
Current Pharmaceutical Design Control of Autoimmune Diseases by the B7-CD28 Family Molecules
Current Pharmaceutical Design Update to: The Aryl Hydrocarbon Receptor in Anticancer Drug Discovery: Friend or Foe?
Medicinal Chemistry Reviews - Online (Discontinued) CBP-dependent Wnt/β-catenin signaling is crucial in regulation of MDR1 transcription
Current Cancer Drug Targets Therapeutic Strategies in Parkinsons Disease
Recent Patents on Endocrine, Metabolic & Immune Drug Discovery Dihidro-β-Agarofuran Sesquiterpenes: A New Class of Reversal Agents of the Multidrug Resistance Phenotype Mediated by P-Glycoprotein in the Protozoan Parasite Leishmania
Current Pharmaceutical Design Recent Patents Reveal Microtubules as Persistent Promising Target for Novel Drug Development for Cancers
Recent Patents on Anti-Infective Drug Discovery Psychological Sequelae of Ovarian Cancer Screening and Genetic Testing for Ovarian Cancer Susceptibility
Current Women`s Health Reviews Binding of a bcl-2 Family Inhibitor to Bovine Serum Albumin: Fluorescence Quenching and Molecular Docking Study
Protein & Peptide Letters Editorial: Targeting Neuregulin1 and HER Receptor Tyrosine Kinases for Therapy of Breast Cancer and Heart Failure
Current Pharmaceutical Design