Abstract
Currently, receptor based radiopharmaceuticals have received great attention in molecular imaging and radiotherapy of cancer, and provide a unique tool for target-specific delivery of radionuclides to pathological tissues. In this context, receptor binding peptides represent an attractive class of target vectors for Nuclear Medicine purposes. The rich chemistry of the group 7 elements elaborated in past years, has allowed the development of different procedures for the preparation of radiolabeled peptides in high yield. This, joint to the use of solid-phase peptide synthesis, has opened the possibility to explore new strategies for approaching the design of new class of radiolabeled receptor-targeted peptides, and to create new versatilities in targeting vehicle design e.g. in synthesis of metal-cyclized peptides or of multivalent targeting agents.
This review provides an overview on several aspects of the development of new 99mTc/188Re-peptide based target specific radiopharmaceuticals, in particular on the synthetic strategies employed for modifying molecular vectors, and the application of the different metal-cores and/or building block for preparing high specific activity agents.
Keywords: Technetium, Rhenium, Peptide, Theragnostic, Maximum Tolerated Dose, RADIOLABELED PEPTIDES, Target-Molecules, Direct Labeling, octapeptide lanreotide, Phosphine
Anti-Cancer Agents in Medicinal Chemistry
Title:Chelating Systems for 99mTc/188Re in the Development of Radiolabeled Peptide Pharmaceuticals
Volume: 12 Issue: 5
Author(s): Cristina Bolzati, Davide Carta, Nicola Salvarese and Fiorenzo Refosco
Affiliation:
Keywords: Technetium, Rhenium, Peptide, Theragnostic, Maximum Tolerated Dose, RADIOLABELED PEPTIDES, Target-Molecules, Direct Labeling, octapeptide lanreotide, Phosphine
Abstract: Currently, receptor based radiopharmaceuticals have received great attention in molecular imaging and radiotherapy of cancer, and provide a unique tool for target-specific delivery of radionuclides to pathological tissues. In this context, receptor binding peptides represent an attractive class of target vectors for Nuclear Medicine purposes. The rich chemistry of the group 7 elements elaborated in past years, has allowed the development of different procedures for the preparation of radiolabeled peptides in high yield. This, joint to the use of solid-phase peptide synthesis, has opened the possibility to explore new strategies for approaching the design of new class of radiolabeled receptor-targeted peptides, and to create new versatilities in targeting vehicle design e.g. in synthesis of metal-cyclized peptides or of multivalent targeting agents.
This review provides an overview on several aspects of the development of new 99mTc/188Re-peptide based target specific radiopharmaceuticals, in particular on the synthetic strategies employed for modifying molecular vectors, and the application of the different metal-cores and/or building block for preparing high specific activity agents.
Export Options
About this article
Cite this article as:
Bolzati Cristina, Carta Davide, Salvarese Nicola and Refosco Fiorenzo, Chelating Systems for 99mTc/188Re in the Development of Radiolabeled Peptide Pharmaceuticals, Anti-Cancer Agents in Medicinal Chemistry 2012; 12 (5) . https://dx.doi.org/10.2174/187152012800617821
DOI https://dx.doi.org/10.2174/187152012800617821 |
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
-
The Growth Hormone Secretagogue Receptor (Ghs-R)
Current Pharmaceutical Design The Protein Kinase Inhibitor Balanol: Structure – Activity Relationships and Structure-Based Computational Studies
Anti-Cancer Agents in Medicinal Chemistry Regulation of MET Receptor Signaling by SOCS1 and its Implications for Hepatocellular Carcinoma
Current Pharmaceutical Design Reviewing the Role of Resveratrol as a Natural Modulator of Microglial Activities
Current Pharmaceutical Design Medication Conveyance Through Nose: Factors Affecting and Novel Applications
Drug Delivery Letters An Update on Circumventing Multidrug Resistance in Cancer by Targeting P-Glycoprotein
Current Cancer Drug Targets Nicotinamide Phosphoribosyltransferase (NAMPT) Inhibitors as Therapeutics: Rationales, Controversies, Clinical Experience
Current Drug Targets Anti-Cancer Drug Design Using Natural and Synthetic Pharmacophores
Current Organic Chemistry Colchicine, Biologic Agents and More for the Treatment of Familial Mediterranean Fever. The Old, the New, and the Rare
Current Medicinal Chemistry Lactobacillus rhamnosus GG Influences Polyamine Metabolism in HGC-27 Gastric Cancer Cell Line: A Strategy Toward Nutritional Approach to Chemoprevention of Gastric Cancer
Current Pharmaceutical Design Hepatocellular Carcinoma Diagnostics, Treatments and Potential Theragnostics in the Asia-Pacific
Current Pharmacogenomics and Personalized Medicine Capillary Electrophoresis with Mass Spectrometry: Applications to Metabolomic Analysis
Current Metabolomics Applications of FDG-PET/CT in Assessment of Vascular Infection and Inflammation
Current Molecular Imaging (Discontinued) Saccharomyces Cerevisiae as a Genetic Model in Anticancer Therapy
Current Pharmacogenomics Based on Nucleotides Analysis of Tumor Cell Lines to Construct and Validate a Prediction Model of Mechanisms of Chemotherapeutics
Anti-Cancer Agents in Medicinal Chemistry Positron Emission Tomography and Computer Tomography (PET/CT) in Prostate, Bladder, and Testicular Cancers
Current Medicinal Chemistry Arachidonic Acid Cascade Enzyme Inhibition and Cancer
Current Enzyme Inhibition Polyphyllin D - A Potential Anti-Cancer Agent to Kill Hepatocarcinoma Cells with Multi-Drug Resistance
Current Chemical Biology 1,2,4-Triazoles: A Review of Synthetic Approaches and the Biological Activity
Letters in Organic Chemistry Gallium-68 in Medical Imaging
Current Radiopharmaceuticals