Radiopharmacologist's and Radiochemist's View on Targeting the Eph/Ephrin Receptor Tyrosine Kinase System

ACS Omega
Christin NeuberJens Pietzsch

Abstract

In the past decade, there have been extensive efforts to open up the Eph/ephrin subfamily of the receptor tyrosine kinase family for diagnostic and therapeutic applications. Besides classical pharmaceutical developments, which focus either on drugs targeting the extracellular ligand binding domains or on the intracellular tyrosine kinase domains of these receptors, there also have been first radiopharmaceutical approaches. Here the focus is on the development of specific and selective probes for molecular imaging, particularly by means of positron emission tomography, and the functional characterization of the Eph/ephrin subfamily in certain target tissues. The aim of this mini-review is to summarize the different approaches toward Eph-targeting radiotracers by using antibodies, peptides, and small molecules and to discuss their radiopharmacological characterization. With regard to the small molecules, further considerations will focus on the design and synthesis of nonradioactive reference compounds and precursors as well as on radiolabeling strategies.

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Citations

Nov 7, 2020·Molecules : a Journal of Synthetic Chemistry and Natural Product Chemistry·Christin NeuberJens Pietzsch

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Methods Mentioned

BETA
imaging technique
xenografts
phage display
fluorescence imaging
xenograft

Clinical Trials Mentioned

NCT04091867
NCT01591356
NCT01642342
NCT04033432
NCT02004717
NCT02219711
NCT01149434
NCT00796055
NCT03374943

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