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

Albertus W. Hensbergen | Zendy; Danny M. van Willigen | Zendy; Florian van Beurden | Zendy; Pim J. van Leeuwen | Zendy; Tessa Buckle | Zendy; Margret Schottelius | Zendy; Tobias Maurer | Zendy; HansJürgen Wester | Zendy; Fijs W. B. van Leeuwen | Zendy

Open Access

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

Author(s) -

Albertus W. Hensbergen,

Danny M. van Willigen,

Florian van Beurden,

Pim J. van Leeuwen,

Tessa Buckle,

Margret Schottelius,

Tobias Maurer,

HansJürgen Wester,

Fijs W. B. van Leeuwen

Publication year - 2019

Publication title -

bioconjugate chemistry

Language(s) - English

Resource type - Journals

SCImago Journal Rank - 1.279

H-Index - 172

eISSN - 1520-4812

pISSN - 1043-1802

DOI - 10.1021/acs.bioconjchem.9b00758

Subject(s) - glutamate carboxypeptidase ii , chemistry , prostate cancer , positron emission tomography , in vivo , transmembrane protein , molecular imaging , image guided surgery , prostate , antigen , in vitro , cancer research , nuclear medicine , cancer , radiology , medicine , biochemistry , immunology , receptor , microbiology and biotechnology , biology

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).

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