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
-
Experimental Benefits of Sex Hormones on Vascular Function and the Outcome of Hormone Therapy in Cardiovascular Disease
Current Cardiology Reviews Kit: Molecule of Interest for the Diagnosis and Treatment of Mastocytosis and other Neoplastic Disorders
Current Cancer Drug Targets Antitumor Activity of Titanocene Y in Xenografted PC3 Tumors in Mice
Letters in Drug Design & Discovery Obesity-Enhanced Colon Cancer: Functional Food Compounds and their Mechanisms of Action
Current Cancer Drug Targets Editorial (Thematic Issue: Endoplasmic Reticulum Stress and Mitochondrial Dysfunction in Diseases: Molecular Targets)
Current Pharmaceutical Design Green Tea Catechins as Novel Antitumor and Antiangiogenic Compounds
Current Medicinal Chemistry - Anti-Cancer Agents Role of Inflammatory Mediators in Angiogenesis
Current Drug Targets - Inflammation & Allergy Use of microRNAs as Anti-Atherosclerosis
Mini-Reviews in Medicinal Chemistry Hydroxytyrosol: Emerging Trends in Potential Therapeutic Applications
Current Pharmaceutical Design Inhaled Corticosteroids in COPD: Pros and Cons
Current Drug Targets Developmental Expression of the Translocator Protein 18 kDa (TSPO) in Testicular Germ Cells
Current Molecular Medicine Taxane Induced Cystoid Macular Edema: Case Report and Integrated Pathogenic Theory
Current Drug Safety Local Melatonin Regulates Inflammation Resolution: A Common Factor in Neurodegenerative, Psychiatric and Systemic Inflammatory Disorders
CNS & Neurological Disorders - Drug Targets Editorial [Continue the Great Journey of Success!]
Current Molecular Medicine The Cholinergic Potential, the Vagus Nerve and Challenges in Treatment of Traumatic Brain Injury
Current Pharmaceutical Design Should the Incorporation of Structural Alerts be Restricted in Drug Design? An Analysis of Structure-Toxicity Trends with Aniline-Based Drugs
Current Medicinal Chemistry The Role of Organic Transporters in Pharmacokinetics and Nephrotoxicity of Newer Antiviral Therapies for HIV and Hepatitis C
Current Drug Metabolism Integrating Virtual Screening and Combinatorial Chemistry for Accelerated Drug Discovery
Combinatorial Chemistry & High Throughput Screening Effects of Intermittent Hypoxia on Expression of Glucose Metabolism Genes in MCF7 Breast Cancer Cell Line
Current Cancer Drug Targets A Review on Biological Activities and Chemical Synthesis of Hydrazide Derivatives
Current Medicinal Chemistry