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Issue 39, 2019
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Two is better than one: difunctional high-affinity PSMA probes based on a [CpM(CO)3] (M = Re/99mTc) scaffold

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Abstract

More than 10% of all men will be given the diagnosis “prostate cancer” during their lifetime. Most of the current radio-diagnostic vehicles involve both expensive and localized production with cyclotrons as well as the use of bulky chelators for the radiometal. We report the use of a new multifunctional cyclopentadiene (Cp) platform to prepare difunctional and monofunctional, PSMA-targeting rhenium and technetium-99m complexes. The Cp-complexes and the free ligands are prepared by straightforward functionalization with either one or two Lys-urea-Glu (LuG) PSMA binding motifs. Cell binding assays revealed that the difunctional rhenium complex displays a dissociation constant (KD = 2.1 nM) that is an order of magnitude lower than the monofunctional compound (KD = 24.2 nM). The 99mTc complexes can be prepared in one step and ≤15 min in high yields. These difunctional Cp-Re(I)/99mTc(I) complexes represent a new class of imaging agents with binding affinities comparable to clinically evaluated compounds. Additionally, this study demonstrates that the Cp-platform can readily be derivatized with amine-containing biomolecules. Extending this work to incorporate both targeting and therapeutic moieties could lead to theranostic systems with Re/99mTc.

Graphical abstract: Two is better than one: difunctional high-affinity PSMA probes based on a [CpM(CO)3] (M = Re/99mTc) scaffold

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Publication details

The article was received on 14 Jun 2019, accepted on 16 Sep 2019 and first published on 16 Sep 2019


Article type: Communication
DOI: 10.1039/C9DT02506E
Dalton Trans., 2019,48, 14600-14605

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    Two is better than one: difunctional high-affinity PSMA probes based on a [CpM(CO)3] (M = Re/99mTc) scaffold

    A. Frei, E. Fischer, B. C. Childs, J. P. Holland and R. Alberto, Dalton Trans., 2019, 48, 14600
    DOI: 10.1039/C9DT02506E

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