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Molecules 2014, 19(12), 20536-20556; doi:10.3390/molecules191220536

18F-Labeled Peptides: The Future Is Bright

Department of Oncology, University of Alberta, 11560 University Avenue, Edmonton, AB T6G 1Z2, Canada
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Received: 22 October 2014 / Revised: 24 November 2014 / Accepted: 28 November 2014 / Published: 8 December 2014
(This article belongs to the Special Issue Peptide Chemistry)
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Abstract

Radiolabeled peptides have been the subject of intense research efforts for targeted diagnostic imaging and radiotherapy over the last 20 years. Peptides offer several advantages for receptor imaging and targeted radiotherapy. The low molecular weight of peptides allows for rapid clearance from the blood and non-target tissue, which results in favorable target-to-non-target ratios. Moreover, peptides usually display good tissue penetration and they are generally non-immunogenic. A major drawback is their potential low metabolic stability. The majority of currently used radiolabeled peptides for targeted molecular imaging and therapy of cancer is labeled with various radiometals like 99mTc, 68Ga, and 177Lu. However, over the last decade an increasing number of 18F-labeled peptides have been reported. Despite of obvious advantages of 18F like its ease of production in large quantities at high specific activity, the low β+ energy (0.64 MeV) and the favorable half-life (109.8 min), 18F-labeling of peptides remains a special challenge. The first part of this review will provide a brief overview on chemical strategies for peptide labeling with 18F. A second part will discuss recent technological advances for 18F-labeling of peptides with special focus on microfluidic technology, automation, and kit-like preparation of 18F-labeled peptides. View Full-Text
Keywords: fluorine-18; peptides; labeling chemistry; microfluidic; automation; PET fluorine-18; peptides; labeling chemistry; microfluidic; automation; PET
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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. (CC BY 4.0).

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Richter, S.; Wuest, F. 18F-Labeled Peptides: The Future Is Bright. Molecules 2014, 19, 20536-20556.

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