Image-Guided Surgery: Are We Getting the Most out of Small-Molecule Prostate-Specific-Membrane-Antigen-Targeted Tracers?

Albertus Wijnand Hensbergen, Danny M. Van Willigen, Florian Van Beurden, Pim J. Van Leeuwen, Tessa Buckle, Margret Schottelius, Tobias Maurer, Hans Jürgen Wester, Fijs W.B. Van Leeuwen

Research output: Contribution to journalArticlepeer-review

44 Scopus citations

Abstract

Expressed on virtually all prostate cancers and their metastases, the transmembrane protein prostate-specific membrane antigen (PSMA) provides a valuable target for the imaging of prostate cancer. Not only does PSMA provide a target for noninvasive diagnostic imaging, e.g., PSMA-positron emission tomography (PSMA-PET), it can also be used to guide surgical resections of PSMA-positive lesions. The latter characteristic has led to the development of a plethora of PSMA-targeted tracers, i.e., radiolabeled, fluorescent, or hybrid. With image-guided surgery applications in mind, this review discusses these compounds based on clinical need. Here, the focus is on the chemical aspects (e.g., imaging label, spacer moiety, and targeting vector) and their impact on in vitro and in vivo tracer characteristics (e.g., affinity, tumor uptake, and clearance pattern).

Original languageEnglish
Pages (from-to)375-395
Number of pages21
JournalBioconjugate Chemistry
Volume31
Issue number2
DOIs
StatePublished - 19 Feb 2020

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