Radiolabeled Small Molecule Protein Kinase Inhibitors for Imaging with PET or SPECT 英文参考文献.docVIP

Molecules 2010, 15, 8260-8278; doi:10.3390/moleculeOPEN ACCESS molecules ISSN 1420-3049 /journal/molecules Review Radiolabeled Small Molecule Protein Kinase Inhibitors for Imaging with PET or SPECT Justin W. Hicks 1, Henry F. VanBrocklin 2, Alan A. Wilson 3, Sylvain Houle 3 and Neil Vasdev 1,3,* 1 Department of Psychiatry, University of Toronto, 250 College St., Toronto, ON M5T 1R8, Canada; E-Mail: justin.hicks@utoronto.ca (J.W.H.) 2 Department of Radiology and Biomedical Imaging, University of California, San Francisco, 185 Berry St., San Francisco, CA 94107, USA; E-Mail: Henry.VanBrocklin@ (H.F.V) 3 PET Centre, Centre for Addiction and Mental Health, 250 College St., Toronto, ON M5T 1R8, Canada; E-Mails: salan.wilson@camhpet.ca (A.A.W.); sylvain.houle@camhpet.ca (S.H.) * Author to whom correspondence should be addressed; E-Mail: neil.vasdev@camhpet.ca; Tel.: +1-416-979-4680; Fax: +1-416-979-4656. Received: 2 November 2010; in revised form: 10 November 2010 / Accepted: 11 November 2010 / Published: 15 November 2010 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 molecule