Abstract
The overexpression of peptide receptors in human tumours makes peptide-ligands attractive agents for the development of specific diagnostic imaging and/or therapy of cancers. Solid-phase peptide synthesis, modern phage display technology and combinatorial peptide chemistry have profoundly affected the pool of available targeting peptides for efficient and specific delivery of imaging or therapeutic label molecules. Additionally, the availability of a wide range of bifunctional chelating agents for the radiolabelling of bioactive peptides with radionuclides has produced a wide variety of useful radiopharmaceutical molecules. This review article examines the principal receptors-binding peptides and their overexpression on tumour cells. We discuss the advantage and the challenges in developing multivalent peptide-based ligands summarising their design strategies and applications.
Keywords: Peptide-receptors, Multivalent approach, Tumour imaging, Cholecystokinin, Metallosilicates, Somatostatin, Vasoactive Intestinal Peptide, Melanocortin Peptides, Bombesin, radiopeptides
Anti-Cancer Agents in Medicinal Chemistry
Title:Peptide-Receptor Ligands and Multivalent Approach
Volume: 12 Issue: 5
Author(s): Paolo Ruzza, Anna Marchiani, Nicola Antolini and Andrea Calderan
Affiliation:
Keywords: Peptide-receptors, Multivalent approach, Tumour imaging, Cholecystokinin, Metallosilicates, Somatostatin, Vasoactive Intestinal Peptide, Melanocortin Peptides, Bombesin, radiopeptides
Abstract: The overexpression of peptide receptors in human tumours makes peptide-ligands attractive agents for the development of specific diagnostic imaging and/or therapy of cancers. Solid-phase peptide synthesis, modern phage display technology and combinatorial peptide chemistry have profoundly affected the pool of available targeting peptides for efficient and specific delivery of imaging or therapeutic label molecules. Additionally, the availability of a wide range of bifunctional chelating agents for the radiolabelling of bioactive peptides with radionuclides has produced a wide variety of useful radiopharmaceutical molecules. This review article examines the principal receptors-binding peptides and their overexpression on tumour cells. We discuss the advantage and the challenges in developing multivalent peptide-based ligands summarising their design strategies and applications.
Export Options
About this article
Cite this article as:
Ruzza Paolo, Marchiani Anna, Antolini Nicola and Calderan Andrea, Peptide-Receptor Ligands and Multivalent Approach, Anti-Cancer Agents in Medicinal Chemistry 2012; 12 (5) . https://dx.doi.org/10.2174/187152012800617849
DOI https://dx.doi.org/10.2174/187152012800617849 |
Print ISSN 1871-5206 |
Publisher Name Bentham Science Publisher |
Online ISSN 1875-5992 |
Call for Papers in Thematic Issues
Induction of cell death in cancer cells by modulating telomerase activity using small molecule drugs
Telomeres are distinctive but short stretches present at the corners of chromosomes and aid in stabilizing chromosomal makeup. Resynthesis of telomeres supported by the activity of reverse transcriptase ribonucleoprotein complex telomerase. There is no any telomerase activity in human somatic cells, but the stem cells and germ cells undergone telomerase ...read more
Role of natural compounds as anti anti-cancer agents
Cancer is considered the leading cause of worldwide mortality, accounting for nearly 10 million deaths in 2022. Cancer outcome can be improved through an appropriate screening and early detection and through an efficient clinical treatment. Chemotherapy remains an important approach in treatment o f several types of cancers, even though ...read more
Signaling and enzymatic modulators in cancer treatment
Cancer accounts for nearly 10 million deaths in 2022 and is considered the leading cause of worldwide mortality. Cancer outcome can be improved through an appropriate screening and early detection and through an efficient clinical treatment. Chemotherapy, radiotherapy and surgery are the most important approach for the treatment of several ...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
Related Articles
-
Heterologous Production of Death Ligands’ and Death Receptors’ Extracellular Domains: Structural Features and Efficient Systems
Protein & Peptide Letters Glioma and Neurokinin-1 Receptor Antagonists: A New Therapeutic Approach
Anti-Cancer Agents in Medicinal Chemistry Calcium Channels and Prostate Cancer
Recent Patents on Anti-Cancer Drug Discovery Pharmacodynamics of Memantine: An Update
Current Neuropharmacology Eph Receptors as Drug Targets: Single-Chain Antibodies and Beyond
Current Drug Targets Alpha-Particle Microdosimetry
Current Radiopharmaceuticals Targeting Brain Tumors with Nanomedicines: Overcoming Blood Brain Barrier Challenges
Current Clinical Pharmacology Oligomerization of G Protein-Coupled Receptors: Biochemical and Biophysical Methods
Current Medicinal Chemistry Proinflammatory Cytokines in Breast Cancer: Mechanisms of Action and Potential Targets for Therapeutics
Current Drug Targets EGFR-Targeting Monoclonal Antibodies in Head and Neck Cancer
Current Cancer Drug Targets Clinical Experience with Antiangiogenic Therapy in Leukemia
Current Cancer Drug Targets Mitochondrial VDAC1: Function in Cell Life and Death and a Target for Cancer Therapy
Current Medicinal Chemistry Concentration-Dependent Bimodal Effect of Specific 18 kDa Translocator Protein (TSPO) Ligands on Cell Death Processes Induced by Ammonium Chloride: Potential Implications for Neuropathological Effects Due to Hyperammonemia
CNS & Neurological Disorders - Drug Targets Advances in Nanomedicine Towards Clinical Application in Oncology and Immunology
Current Pharmaceutical Biotechnology Intraoperative Magnetic Resonance Imaging
Current Medical Imaging Microarray Technologies for Intracellular Kinome Analysis
Current Medicinal Chemistry Biologically Active Peptides Interacting with the G Protein-Coupled Formylpeptide Receptors
Protein & Peptide Letters A Review on Novel Breast Cancer Therapies: Photodynamic Therapy and Plant Derived Agent Induced Cell Death Mechanisms
Anti-Cancer Agents in Medicinal Chemistry Opioids and the Blood-Brain Barrier: A Dynamic Interaction with Consequences on Drug Disposition in Brain
Current Neuropharmacology Spin Trapping: An Essential Tool for the Study of Diseases Caused by Oxidative Stress
Current Topics in Medicinal Chemistry