Abstract
Multimerization offers unique kinetic and thermodynamic properties to molecules. Multimeric ligands, characterized by multiple similar or different monomeric molecules tethered together, can bind several receptors simultaneously. Multimerization occurs also in nature. This process can be used to develop molecules with high diagnostic and therapeutic value. By altering parameters as linkers` length and flexibility, scaffold and backbones insertion, and ligands-receptors recognition, it is possible to provide high selectivity and binding affinity. The resultant multimeric ligand has a more favorable binding affinity than corresponding monomeric ligands.
Keywords: Multimerization, binding, avidity, cooperativity, valency, ligand design, nuclear imaging, nanotechnology
Current Pharmaceutical Design
Title:Multimerization Improves Targeting of Peptide Radio-Pharmaceuticals
Volume: 18 Issue: 17
Author(s): Giuseppe Carlucci, Hildo J.K. Ananias, Zilin Yu, Christophe Van de Wiele, Rudi A. Dierckx, Igle J. de Jong and Philip H. Elsinga
Affiliation:
Keywords: Multimerization, binding, avidity, cooperativity, valency, ligand design, nuclear imaging, nanotechnology
Abstract: Multimerization offers unique kinetic and thermodynamic properties to molecules. Multimeric ligands, characterized by multiple similar or different monomeric molecules tethered together, can bind several receptors simultaneously. Multimerization occurs also in nature. This process can be used to develop molecules with high diagnostic and therapeutic value. By altering parameters as linkers` length and flexibility, scaffold and backbones insertion, and ligands-receptors recognition, it is possible to provide high selectivity and binding affinity. The resultant multimeric ligand has a more favorable binding affinity than corresponding monomeric ligands.
Export Options
About this article
Cite this article as:
Carlucci Giuseppe, J.K. Ananias Hildo, Yu Zilin, Van de Wiele Christophe, A. Dierckx Rudi, J. de Jong Igle and H. Elsinga Philip, Multimerization Improves Targeting of Peptide Radio-Pharmaceuticals, Current Pharmaceutical Design 2012; 18 (17) . https://dx.doi.org/10.2174/13816128112092501
DOI https://dx.doi.org/10.2174/13816128112092501 |
Print ISSN 1381-6128 |
Publisher Name Bentham Science Publisher |
Online ISSN 1873-4286 |
Call for Papers in Thematic Issues
"Tuberculosis Prevention, Diagnosis and Drug Discovery"
The Nobel Prize-winning discoveries of Mycobacterium tuberculosis and streptomycin have enabled an appropriate diagnosis and an effective treatment of tuberculosis (TB). Since then, many newer diagnosis methods and drugs have been saving millions of lives. Despite advances in the past, TB is still a leading cause of infectious disease mortality ...read more
Current Pharmaceutical challenges in the treatment and diagnosis of neurological dysfunctions
Neurological dysfunctions (MND, ALS, MS, PD, AD, HD, ALS, Autism, OCD etc..) present significant challenges in both diagnosis and treatment, often necessitating innovative approaches and therapeutic interventions. This thematic issue aims to explore the current pharmaceutical landscape surrounding neurological disorders, shedding light on the challenges faced by researchers, clinicians, and ...read more
Emerging and re-emerging diseases
Faced with a possible endemic situation of COVID-19, the world has experienced two important phenomena, the emergence of new infectious diseases and/or the resurgence of previously eradicated infectious diseases. Furthermore, the geographic distribution of such diseases has also undergone changes. This context, in turn, may have a strong relationship with ...read more
Melanoma and Non-Melanoma Skin Cancer Treatment: Standard of Care and Recent Advances
In this thematic issue, we aim to provide a standard of care of the diagnosis and treatment of melanoma and non-melanoma skin cancer. The editor will invite authors from different countries who will write review articles of melanoma and non-melanoma skin cancers. The Diagnosis, Staging, Surgical Treatment, Non-Surgical Treatment all ...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
-
Age-Related Pharmacokinetic and Pharmacodynamic Changes and Related Risk of Adverse Drug Reactions
Current Medicinal Chemistry IL-22 and Its Receptors, New Players in the Inflammatory Network
Anti-Inflammatory & Anti-Allergy Agents in Medicinal Chemistry Metabolism in Patients with Rheumatoid Arthritis: Resting Energy Expenditure, Physical Activity and Diet-Induced Thermogenesis. Invited Review
Recent Patents on Endocrine, Metabolic & Immune Drug Discovery Research Progress of Exogenous Plant MiRNAs in Cross-Kingdom Regulation
Current Bioinformatics Modulation of Tumour-Related Signaling Pathways by Natural Pentacyclic Triterpenoids and their Semisynthetic Derivatives
Current Medicinal Chemistry Glycyrrhetinic Acid and Its Derivatives: Anti-Cancer and Cancer Chemopreventive Properties, Mechanisms of Action and Structure- Cytotoxic Activity Relationship
Current Medicinal Chemistry Can We Select Patients for Colorectal Cancer Prevention with Aspirin?
Current Pharmaceutical Design PET Tracers for Serotonin Receptors and Their Applications
Central Nervous System Agents in Medicinal Chemistry Role of Mitochondrial Translocator Protein (18 kDa) on Mitochondrial- Related Cell Death Processes
Recent Patents on Endocrine, Metabolic & Immune Drug Discovery Oxycodone/Naloxone in the Management of Patients with Pain and Opioid–Induced Bowel Dysfunction
Current Drug Targets Genetics and Ulcerative Colitis: What are the Clinical Implications?
Current Drug Targets Targeted Elimination of Leukemia Stem Cells; a New Therapeutic Approach in Hemato-Oncology
Current Drug Targets Dual Role of Heat Shock Proteins (HSPs) in Anti-Tumor Immunity
Current Molecular Medicine Fluorescent Molecular Imaging: Technical Progress and Current Preclinical and Clinical Applications in Urogynecologic Diseases
Current Molecular Medicine Vanilloid Receptor Antagonists: Emerging Class of Novel Anti-Inflammatory Agents for Pain Management
Current Pharmaceutical Design Neurokinin Receptors as Potential Targets in Breast Cancer Treatment
Current Drug Discovery Technologies Recent Development of Copolymeric Nano-Drug Delivery System for Paclitaxel
Anti-Cancer Agents in Medicinal Chemistry Opportunities and Challenges in Nano-structure Mediated Drug Delivery: Where Do We Stand?
Current Nanomedicine Nanoparticles: A Neurotoxicological Perspective
CNS & Neurological Disorders - Drug Targets A Micro-Aggregation Algorithm Based on Density Partition Method for Anonymizing Biomedical Data
Current Bioinformatics