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
-
Steroids and the Endometrium
Current Medicinal Chemistry Treatment of High-Grade Pelvic-Type Serous Carcinomas (Ovary, Fallopian Tube and Peritoneum): Current Therapeutic Paradigms, Prospects, and Challenges
Current Cancer Therapy Reviews A Ferrocene Derivative Reduces Cisplatin Resistance in Breast Cancer Cells through Suppression of MDR-1 Expression and Modulation of JAK2/STAT3 Signaling Pathway
Anti-Cancer Agents in Medicinal Chemistry The Concept of Titration can be Transposed to Fluid Management. But does is Change the Volumes? Randomised Trial on Pleth Variability Index During Fast-Track Colonic Surgery
Current Clinical Pharmacology Targeting Telomerase for Cancer Therapy
Current Cancer Therapy Reviews Non-Pharmacologic Strategies in Hematopoietic Stem Cell Transplantation
Current Pharmaceutical Design Vitamin-D in the Immune System: Genomic and Non-Genomic Actions
Mini-Reviews in Medicinal Chemistry Rationale for an Intraperitoneal Gemcitabine Chemotherapy Treatment for Patients with Resected Pancreatic Cancer
Recent Patents on Anti-Cancer Drug Discovery Biodegradable Nanoparticles: A Recent Approach and Applications
Current Drug Targets Exfoliated Epithelial Cells: A Non-Invasive way to Evaluate the Physiological State of Gastrointestinal Epithelium
Recent Patents on Biomedical Engineering (Discontinued) Epigenetic Therapies of Cancer
Current Cancer Therapy Reviews Paucimorphic Alleles versus Polymorphic Alleles and Rare Mutations in Disease Causation: Theory, Observation and Detection
Current Genomics Personalized Peptide-based Vaccination for Treatment of Colorectal Cancer: Rational and Progress
Current Drug Targets Diagnosis, Pathogenesis and Therapeutic Targets in Amyotrophic Lateral Sclerosis
CNS & Neurological Disorders - Drug Targets Role of α7-Nicotinic Acetylcholine Receptor in Normal and Cancer Stem Cells
Current Drug Targets Dysregulation of RNA Mediated Gene Expression in Motor Neuron Diseases
CNS & Neurological Disorders - Drug Targets A Primary Reduced TCA Flux Governs Substrate Oxidation in T2D Skeletal Muscle
Current Diabetes Reviews Triterpene Derivatives as Inhibitors of Protein Involved in the Inflammatory Process: Molecules Interfering with Phospholipase A2, Cycloxygenase, and Lipoxygenase
Current Drug Targets Imaging Virus-Associated Cancer
Current Pharmaceutical Design The Relevance of Microdialysis for Clinical Oncology
Current Clinical Pharmacology