Copper chelation chemistry and its role in copper radiopharmaceuticals

T J Wadas; E H Wong; G R Weisman; C J Anderson

doi:10.2174/138161207779313768

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Copper chelation chemistry and its role in copper radiopharmaceuticals

Journal article

Peer reviewed

Copper chelation chemistry and its role in copper radiopharmaceuticals

T J Wadas, E H Wong, G R Weisman and C J Anderson

Current pharmaceutical design, Vol.13(1), pp.3-16

2007

DOI: 10.2174/138161207779313768

PMID: 17266585

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Abstract

Molecular imaging is an important scientific discipline that plays a major role in clinical medicine and pharmaceutical development. While several imaging modalities including X-ray computed tomography (CT) and magnetic resonance imaging (MRI) generate high-resolution anatomical images, positron emission tomography (PET) and single photon emission computed tomography (SPECT) offer insight into the physiological processes that occur within a living organism. Of these two nuclear medicine imaging techniques, PET has advantages with respect to sensitivity and resolution, and this has led to the production and development of many positron emitting radionuclides that include non-traditional radionuclides of the transition metals. Copper-64 (t(1/2) = 12.7 h, beta(+): 17.4%, E(beta+max) = 656 keV; beta(-): 39%, E(beta-max) = 573 keV) has emerged as an important positron emitting radionuclide that has the potential for use in diagnostic imaging and radiotherapy. However, (64)Cu must be delivered to the living system as a stable complex that is attached to a biological targeting molecule for effective imaging and therapy. Therefore, significant research has been devoted to the development of ligands that can stably chelate (64)Cu. This review discusses the necessary characteristics of an effective (64)Cu chelator, while highlighting the development and evaluation of (64)Cu-complexes attached to biologically-targeted ligands.

Animals

Chelating Agents - chemistry

Copper Radioisotopes - chemistry

Cyclohexylamines - chemistry

Dipeptides - chemical synthesis

Drug Design

Drug Stability

Heterocyclic Compounds - chemistry

Humans

Ligands

Molecular Structure

Positron-Emission Tomography

Radiopharmaceuticals - chemical synthesis

Radiopharmaceuticals - chemistry

Details

Title: Subtitle: Copper chelation chemistry and its role in copper radiopharmaceuticals
Creators: T J Wadas - Mallinckrodt Institute of Radiology, Washington University School of Medicine, 510 S. Kingshighway Blvd., Campus Box 8225, St. Louis, MO 63110, USA.
E H Wong
G R Weisman
C J Anderson
Resource Type: Journal article
Publication Details: Current pharmaceutical design, Vol.13(1), pp.3-16
DOI: 10.2174/138161207779313768
PMID: 17266585
ISSN: 1381-6128
eISSN: 1873-4286
Grant note: F32 CA115148 / NCI NIH HHS R01 CA093375 / NCI NIH HHS
Language: English
Date published: 2007
Academic Unit: Radiology; Radiation Oncology
Record Identifier: 9984313073102771

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