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
-
Three-Dimensional Manufactured Supports for Breast Cancer Stem Cell Population Characterization
Current Drug Targets Longitudinal Melatonin Production in Female Laboratory Rats During 1997-2006: Possible Modulatory Effects of Changing Solar Activity
Current Aging Science Photosensitive Precursors to Nitric Oxide
Current Topics in Medicinal Chemistry Fentanyl for Breakthrough Cancer Pain: Where are We?
Reviews on Recent Clinical Trials Analysis of Microarray Gene Expression Data
Current Bioinformatics Selective Induction of Apoptosis: Promising Therapy in Pancreatic Cancer
Current Pharmaceutical Design Therapeutic Potential of High Mobility Group Box-1 in Ischemic Injury and Tissue Regeneration
Current Vascular Pharmacology From Gut Homeostasis to Cancer
Current Molecular Medicine Pharmacogenetic Variation and Metformin Response
Current Drug Metabolism Designing an Expert System for the Diagnosis of Multiple Myeloma by Using Rough Set Theory
Recent Advances in Computer Science and Communications Prediction of Bioactive Compound Pathways Using Chemical Interaction and Structural Information
Combinatorial Chemistry & High Throughput Screening Thalidomide Metabolism and Hydrolysis: Mechanisms and Implications
Current Drug Metabolism Characterization and Management of Cutaneous Side Effects Related to the Immunosuppressive Treatment in Solid Organ Recipients
Current Drug Targets Non-viral Gene Delivery and Therapeutics Targeting to Brain
Current Nanoscience Caffeine; the Forgotten Potential for Parkinson's Disease
CNS & Neurological Disorders - Drug Targets “Metabolic Aspects” In Inflammatory Bowel Diseases
Current Drug Delivery The Biological Effects of Diagnostic Cardiac Imaging
Current Pharmaceutical Design The Akt/PKB Family of Protein Kinases: A Review of Small Molecule Inhibitors and Progress Towards Target Validation
Current Topics in Medicinal Chemistry COPD Management: Look Beyond the Airway Obstruction, Chronic Bronchitis and Emphysema
Current Respiratory Medicine Reviews Malignant Phyllodes Tumors with Heterologous Sarcomatous Elements Presenting as Hyperechoic Masses on Ultrasonography: A Case Report
Current Medical Imaging