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
-
Cancer Therapy: Targeting Cell Cycle Regulators
Anti-Cancer Agents in Medicinal Chemistry MicroRNAs: Newcomers into the ALS Picture
CNS & Neurological Disorders - Drug Targets Smart Nanocarriers for Targeted Cancer Therapy
Anti-Cancer Agents in Medicinal Chemistry A Proposed Screening Paradigm for Discovery of Covalent Inhibitor Drugs
Drug Metabolism Letters Proteasome Inhibitors and Modulators of Angiogenesis in Multiple Myeloma
Current Medicinal Chemistry The Molecular and Pharmacological Mechanisms of HIV-Related Neuropathic Pain
Current Neuropharmacology Mast Cells and Basophils: Trojan Horses of Conventional Lin- Stem/Progenitor Cell Isolates
Current Pharmaceutical Design Procarbazine – A Traditional Drug in the Treatment of Malignant Gliomas
Current Medicinal Chemistry Inhibitory Effect of Hydroxysafflor Yellow B on the Proliferation of Human Breast Cancer MCF-7 Cells
Recent Patents on Anti-Cancer Drug Discovery GMDR: Versatile Software for Detecting Gene-Gene and Gene-Environment Interactions Underlying Complex Traits
Current Genomics Patent Annotations
Recent Patents on CNS Drug Discovery (Discontinued) Urokinase Receptor and Integrin Interactions
Current Pharmaceutical Design Hepatocellular Carcinoma Detection by Gallium Scan and Subsequent Treatment by Gallium Maltolate: Rationale and Case Study
Anti-Cancer Agents in Medicinal Chemistry Recent Patents on Proteasome Inhibitors of Natural Origin
Recent Patents on Anti-Cancer Drug Discovery Combination Therapies of Artemisinin and its Derivatives as a Viable Approach for Future Cancer Treatment
Current Pharmaceutical Design Quinolones in the Search for New Anticancer Agents
Current Pharmaceutical Design Expression of Specificity Protein Transcription Factors in Pancreatic Cancer and their Association in Prognosis and Therapy
Current Medicinal Chemistry IDO+ DCs and Signalling Pathways
Current Cancer Drug Targets Sphere Formation Assay is not an Effective Method for Cancer Stem Cell Derivation and Characterization from the Caco-2 Colorectal Cell Line
Current Stem Cell Research & Therapy Recent Patents Reveal Microtubules as Persistent Promising Target for Novel Drug Development for Cancers
Recent Patents on Anti-Infective Drug Discovery