Abstract
Since its first description in 1955, tumor hypoxia has become a central issue in cancer treatment. Since then, it is essential to diagnose accurately the tumor oxygenation degree in order to establish the appropriate treatment.
In this regard, a wide diversity of radiopharmaceuticals for in vivo imaging has been developed. Special conditions of the hypoxic microenvironment are low O2 partial pressure, enhanced levels of reductases, and genetic-adaptation-expression biomolecules involved in angiogenesis, erythropoiesis, cellular proliferation, apoptosis, metabolism- and glucose-uptake, local invasion, and metastatic spread. The development of radiolabeled hypoxia markers has been based on reductase substrates, like bioreductive ligands, or on entities capable of recognizing overexpressed proteins under hypoxia conditions, i.e. HIF-1α and carbonic anhydrase IX, among others. In this review these hypoxia markers are analyzed focusing on their medicinal chemistry characteristics.Keywords: Hypoxia, radiopharmaceuticals, imaging.
Anti-Cancer Agents in Medicinal Chemistry
Title:Radiopharmaceuticals in Tumor Hypoxia Imaging: A Review Focused on Medicinal Chemistry Aspects
Volume: 17 Issue: 3
Author(s): Pablo Cabral and Hugo Cerecetto
Affiliation:
Keywords: Hypoxia, radiopharmaceuticals, imaging.
Abstract: Since its first description in 1955, tumor hypoxia has become a central issue in cancer treatment. Since then, it is essential to diagnose accurately the tumor oxygenation degree in order to establish the appropriate treatment.
In this regard, a wide diversity of radiopharmaceuticals for in vivo imaging has been developed. Special conditions of the hypoxic microenvironment are low O2 partial pressure, enhanced levels of reductases, and genetic-adaptation-expression biomolecules involved in angiogenesis, erythropoiesis, cellular proliferation, apoptosis, metabolism- and glucose-uptake, local invasion, and metastatic spread. The development of radiolabeled hypoxia markers has been based on reductase substrates, like bioreductive ligands, or on entities capable of recognizing overexpressed proteins under hypoxia conditions, i.e. HIF-1α and carbonic anhydrase IX, among others. In this review these hypoxia markers are analyzed focusing on their medicinal chemistry characteristics.Export Options
About this article
Cite this article as:
Cabral Pablo and Cerecetto Hugo, Radiopharmaceuticals in Tumor Hypoxia Imaging: A Review Focused on Medicinal Chemistry Aspects, Anti-Cancer Agents in Medicinal Chemistry 2017; 17 (3) . https://dx.doi.org/10.2174/1871520616666160307142514
DOI https://dx.doi.org/10.2174/1871520616666160307142514 |
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
-
Association between Antiretroviral Treatment and Markers of Systemic Inflammation among HIV Patients in Ghana
Current HIV Research Stressing Conditions as Tools to Boost the Biosynthesis of Valuable Plant Natural Products
Recent Patents on Biotechnology Repositioning of HIV Aspartyl Peptidase Inhibitors for Combating the Neglected Human Pathogen Trypanosoma cruzi
Current Medicinal Chemistry Let Them Eat Cake
Current Nutrition & Food Science Kinin Receptors in Vascular Biology and Pathology
Current Vascular Pharmacology Toll-Like Receptors: Link between “Danger” Ligands and Plaque Instability
Current Drug Targets Endothelial Function Assessment in Complicated Hypertension
Current Pharmaceutical Design The Role of Autophagy in the Pathogenesis of Ischemic Stroke
Current Neuropharmacology Analysis of Contrast-Enhanced Intravascular Ultrasound Images for the Assessment of Coronary Plaque Neoangiogenesis: Another Step Closer to the Identification of the Vulnerable Plaque
Current Pharmaceutical Design Modification of Lifestyle Factors are Needed to Improve the Metabolic Health of Patients with Cardiovascular Disease Risk
Current Pharmaceutical Design Single-Pill Triple Fixed Dose Combination Therapy with Single Component Drug Monitoring in Treatment-Resistant Hypertension: A Pilot Study
Current Vascular Pharmacology Protein-protein Interactions: Network Analysis and Applications in Drug Discovery
Current Pharmaceutical Design Leptin in Non-Autoimmune Inflammation
Inflammation & Allergy - Drug Targets (Discontinued) Adipose Tissue: The Link Between Obesity and Cardiovascular Disease
Cardiovascular & Hematological Disorders-Drug Targets Can Life Before Birth Affect Health Ever After?
Current Women`s Health Reviews Discovery Approaches for Novel Dyslipidemia Drugs
Current Drug Discovery Technologies Potentiating the Naturally Occurring Process for Repair of Damaged Heart
Current Pharmaceutical Design Iatrogenic QT Abnormalities and Fatal Arrhythmias: Mechanisms and Clinical Significance
Current Cardiology Reviews Benzothiazole Derivatives: Novel Inhibitors of Methylglyoxal Mediated Glycation of Proteins In Vitro
Medicinal Chemistry Calcific Aortic Stenosis: Molecular and Cellular Mechanisms, Medical Treatment Alternatives
Current Cardiology Reviews