Topical Issue on Bioorthogonal Chemistry applied to the development of the Molecular Imaging
prof. Joaquin Plumet, Complutense University, Spain
Molecular imaging is a type of medical imaging that provides detailed pictures of what is happening inside the body at the molecular and cellular level. Where other diagnostic imaging procedures—such as x-rays, computed tomography (CT) and ultrasound—offer pictures of physical structure, molecular imaging allows physicians to see how the body is functioning and to measure its chemical and biological processes.
Molecular imaging includes the field of nuclear medicine, which uses very small amounts of radioactive materials (radiopharmaceuticals) to diagnose and treat disease. In nuclear medicine imaging, the radiopharmaceuticals are detected by special types of cameras that work with computers to provide very precise pictures of the area of the body being imaged. Nuclear medicine can also be used to treat certain types of cancer and other diseases.
Molecular imaging procedures—which are noninvasive, safe and painless—are used to diagnose and manage the treatment of cancer, heart disease, brain disorders such as Alzheimer’s and Parkinson’s disease, gastrointestinal disorders, lung disorders, bone disorders, kidney and thyroid disorders, and more.
Positron emission tomography (PET) is a nuclear medical imaging technique for quantitative measurement of physiologic parameters in vivo, based on the detection of small amounts of positron-emitter-labelled biologic molecules. Various radiotracers are available for neurological, cardiological, and oncological applications in the clinic and in research protocols.
PET is based on the detection of very small (picomolar) quantities of biological substances which are labelled with a positron emitter. Most commonly used are carbon- 11, oxygen-15, nitrogen-13, and fluorine-18. Advantages of positron labelled substances are their very high specificity (molecular targeting), the possibility of using biological active substances without changing their behaviour by the label, and fulfillment of the tracer principle. Thus, the process of interest remains unchanged during the measurement. Target structures of these molecules are e.g. glucose metabolism, receptor binding potential, catecholamine transport, amino acid transport, or protein synthesis. All the above mentioned nuclides have very short radioactive half-lives (2 min for O-15, 109 min for F-18), which necessitates a nearby cyclotron and radiochemistry facility [Sibylle I. Ziegler. Positron Emission Tomography: Principles, Technology, and Recent Developments. Nuclear Physics A, 2005, 752, 679-687].
In particular, Fluorine-18 is one of the several isotopes of fluorine that is routinely used in radiolabeling of biomolecules for PET because of its positron emitting property and favorable half-life of 109.8 min. The biologically active molecule most commonly used for PET is 2-deoxy -2-18F-fluoro-β-D-glucose (18F-FDG), an analogue of glucose, for early detection of tumors. The concentrations of tracer accumulation (PET image) demonstrate the metabolic activity of tissues in terms of regional glucose metabolism and accumulation. Other tracers are also used in PET to image the tissue concentration [Mian. M. Alauddin. Positron emission tomography (PET) imaging with 18F-based radiotracers. Am. J. Nucl. Med. Mol. Imaging, 2012, 2, 55-76].
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