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Molecules 2010, 15(11), 8260-8278; doi:10.3390/molecules15118260
Review

Radiolabeled Small Molecule Protein Kinase Inhibitors for Imaging with PET or SPECT

1
,
2
,
3
,
3
 and
1,3,*
1 Department of Psychiatry, University of Toronto, 250 College St., Toronto, ON M5T 1R8, Canada 2 Department of Radiology and Biomedical Imaging, University of California, San Francisco, 185 Berry St., San Francisco, CA 94107, USA 3 PET Centre, Centre for Addiction and Mental Health, 250 College St., Toronto, ON M5T 1R8, Canada
* Author to whom correspondence should be addressed.
Received: 2 November 2010 / Revised: 10 November 2010 / Accepted: 11 November 2010 / Published: 15 November 2010
(This article belongs to the Special Issue Radiochemistry)
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Abstract

Imaging protein kinase expression with radiolabeled small molecule inhibitors has been actively pursued to monitor the clinical potential of targeted therapeutics and treatments as well as to determine kinase receptor density changes related to disease progression. The goal of the present review is to provide an overview of the breadth of radiolabeled small molecules that have been synthesized to target intracellular protein kinases, not only for imaging in oncology, but also for other areas of interest, particularly the central nervous system.  Considerable radiotracer development has focused on imaging receptor tyrosine kinases of growth factors, protein kinases A, B and C, and glycogen synthase kinase–3β. Design considerations, structural attributes and relevant biological results are summarized.
Keywords: molecular imaging; protein kinase; small molecules inhibitors; positron emission tomography; single photon emission computer tomography molecular imaging; protein kinase; small molecules inhibitors; positron emission tomography; single photon emission computer tomography
This is an open access article distributed under the Creative Commons Attribution License which permits unrestricted use, distribution, and reproduction in any medium, provided the original work is properly cited.

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Hicks, J.W.; VanBrocklin, H.F.; Wilson, A.A.; Houle, S.; Vasdev, N. Radiolabeled Small Molecule Protein Kinase Inhibitors for Imaging with PET or SPECT. Molecules 2010, 15, 8260-8278.

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