Dataset Information

Absorption- and Excitation-Modulated Luminescence of Pr³⁺, Nd³⁺, and Lu³⁺ Compounds with Dianions of Tetrafluoroterephthalic and Camphoric Acids.

ABSTRACT: The luminescence of coordination polymers of Pr³⁺, Nd³⁺, and Lu³⁺ with tetrafluoroterephthalate and camphorate, [Ln₂(Fbdc)₃(DMF)₂(H₂O)]₂ (Ln = Pr, Nd, Lu) and [Ln₂(Camph)₂(NO₃)₂(MeOH)]₄ (Ln = Pr, Nd, Lu), was studied. Ligand-centered and/or metal-centered emissions appear, which depend on the excitation wavelength, ultimately allowing the emitted light color to be adjusted. Low-efficiency ligand-to-metal energy transfer leads to a difference between the excitation spectra of the tetrafluoroterephthalate- and camphorate-Pr³⁺ compounds, arising from a primary filtering effect on the ligand-centered excitation, by Pr³⁺ absorption. A secondary inner filter effect significantly changes the shape of the luminescence band, allowing a wide variation in the emission color, producing, for instance, a purple color, which is not the normal spectral emission. The low-efficiency energy transfer renders tetrafluoroterephthalate and camphorate ineffective as traditional "antenna" ligands for Pr³⁺ and Nd³⁺.

SUBMITTER: Mikhalyova EA

PROVIDER: S-EPMC6648583 | biostudies-literature | 2019 Feb

REPOSITORIES: biostudies-literature

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Publications

Absorption- and Excitation-Modulated Luminescence of Pr3+, Nd3+, and Lu3+ Compounds with Dianions of Tetrafluoroterephthalic and Camphoric Acids.

Mikhalyova Elena A EA Khomenko Olena V OV Gavrilenko Konstantin S KS Dotsenko Vladimir P VP Addison Anthony W AW Pavlishchuk Vitaly V VV

ACS omega 20190205 2

The luminescence of coordination polymers of Pr3+, Nd3+, and Lu3+ with tetrafluoroterephthalate and camphorate, [Ln2(Fbdc)3(DMF)2(H2O)]2 (Ln = Pr, Nd, Lu) and [Ln2(Camph)2(NO3)2(MeOH)]4 (Ln = Pr, Nd, Lu), was studied. Ligand-centered and/or metal-centered emissions appear, which depend on the excitation wavelength, ultimately allowing the emitted light co ...[more]

PMID: 31459502

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Project description:BackgroundRadiohybrid PSMA-targeted ligands (rhPSMA) have been introduced as a novel platform for theranostic applications. Among a variety of rhPSMA-ligands developed for radioligand therapy, two stereoisomers [177Lu]Lu-rhPSMA-10.1 and -10.2 have been synthesized and initially characterized in preclinical experiments with the aim to provide an optimized binding profile to human serum albumin, a reduction of charge, and thus accelerated kidney excretion, and unaffected or even improved tumor uptake. As both isomers showed similar in vitro characteristics and tumor uptake at 24 h post injection in tumor bearing mice and in order to identify the isomer with the most favorable pharmacokinetics for radioligand therapy, we carried out in-depth biodistribution and dosimetry studies in tumor-bearing and healthy mice.ResultsrhPSMA-10.1 and -10.2 were radiolabeled with lutetium-177 according to the established procedures of other DOTA-based PSMA ligands and displayed a high and comparable stability in all buffers and human serum (> 97%, 24 h). Biodistribution studies revealed fast clearance from the blood pool (0.3-0.6%ID/g at 1 h) and other background tissues within 48 h. Distinctive differences were found in the kidneys, where [177Lu]Lu-rhPSMA-10.1 displayed lower initial uptake and faster excretion kinetics compared to [177Lu]Lu-rhPSMA-10.2 expressed by a 1.5-fold and ninefold lower uptake value at 1 h and 24 h in healthy animals, respectively. Tumor uptake was comparable and in the range of 8.6-11.6%ID/g for both isomers over 24 h and was maintained up to 168 h at a level of 2.2 ± 0.8 and 4.1 ± 1.4%ID/g for [177Lu]Lu-rhPSMA-10.1 and [177Lu]Lu-rhPSMA-10.2, respectively.ConclusionOur preclinical data on biodistribution and dosimetry indicate a more favorable profile of [177Lu]Lu-rhPSMA-10.1 compared to [177Lu]Lu-rhPSMA-10.2 for PSMA-targeted radioligand therapy. [177Lu]Lu-rhPSMA-10.1 shows fast kidney clearance kinetics resulting in excellent tumor-to-organ ratios over a therapy relevant time course. Meanwhile, [177Lu]Lu-rhPSMA-10.1 is currently being investigated in clinical phase I/II studies in patients with mCRPC (NCT05413850), in patients with high-risk localized PC (NCT06066437, Nautilus Trial) and after external beam radiotherapy (NCT06105918).

Dataset Information

Absorption- and Excitation-Modulated Luminescence of Pr³⁺, Nd³⁺, and Lu³⁺ Compounds with Dianions of Tetrafluoroterephthalic and Camphoric Acids.

Publications

Absorption- and Excitation-Modulated Luminescence of Pr<sup>3+</sup>, Nd<sup>3+</sup>, and Lu<sup>3+</sup> Compounds with Dianions of Tetrafluoroterephthalic and Camphoric Acids.

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