Bioconjugate Chemistry, volume 28, issue 9, pages 2485-2492

Improving the Imaging Contrast of 68Ga-PSMA-11 by Targeted Linker Design: Charged Spacer Moieties Enhance the Pharmacokinetic Properties

Baranski Ann-Christin ¹

Schäfer Martin ¹

Bauder-Wüst Ulrike ¹

Wacker Anja ¹

Schmidt Jana ¹

Liolios Christos ¹

Mier Walter ²

Haberkorn Uwe ²

Eisenhut Michael ³

Kopka Klaus ⁴

Eder Matthias ⁵

Hide authors affiliations Show authors affiliations: 5 affiliations

German Cancer Research Center (dkfz

Department of Nuclear Medicine, University of Heidelberg, Im Neuenheimer Feld 400, 69120 Heidelberg, Germany |

Imaging and Radiooncology

⁴

UNIVERSITY OF HEIDELBERG |

⁵

Division of Radiopharmaceutical Development, German Cancer Consortium (DKTK) Freiburg, Department of Nuclear Medicine, Faculty of Medicine, Medical Center − University of Freiburg, Hugstetter Straße 55, 79106 Freiburg, Germany |

Publication type: Journal Article

Publication date: 2017-08-24

American Chemical Society (ACS)

Journal: Bioconjugate Chemistry

Quartile SCImago

Quartile WOS

Impact factor: 4.7

ISSN: 10431802, 15204812

DOI: 10.1021/acs.bioconjchem.7b00458

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Organic Chemistry

Pharmacology

Pharmaceutical Science

Biotechnology

Bioengineering

Biomedical Engineering

Abstract

68Ga-Glu-urea-Lys-(Ahx)-HBED-CC (68Ga-PSMA-11) represents a successful radiopharmaceutical for PET/CT imaging of prostate cancer. Further optimization of the tumor-to-background contrast might significantly enhance the sensitivity of PET/CT imaging and the probability of detecting recurrent prostate cancer at low PSA values. This study describes the advantage of histidine (H)/glutamic acid (E) and tryptophan (W)/glutamic acid (E) containing linkers on the pharmacokinetic properties of 68Ga-PSMA-11. The tracers were obtained by a combination of standard Fmoc-based solid-phase synthesis and copper(I)-catalyzed azide–alkyne cycloaddition. Their 68Ga complexes were compared to the clinical reference 68Ga-PSMA-11 with respect to cell binding, effective internalization, and tumor targeting properties in LNCaP-bearing balb/c nu/nu mice. The introduction of (HE)i (i = 1–3) or (WE)i (i = 1–3) into PSMA-11 resulted in a significantly changed biodistribution profile. The uptake values in kidneys, spleen, liver, and ...

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Citations by publishers

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American Chemical Society (ACS)	American Chemical Society (ACS), 9, 21.43% American Chemical Society (ACS) 9 publications, 21.43%
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CSIRO Publishing	CSIRO Publishing, 1, 2.38% CSIRO Publishing 1 publication, 2.38%
American Association for Cancer Research (AACR)	American Association for Cancer Research (AACR), 1, 2.38% American Association for Cancer Research (AACR) 1 publication, 2.38%
Frontiers Media S.A.	Frontiers Media S.A., 1, 2.38% Frontiers Media S.A. 1 publication, 2.38%
	1 2 3 4 5 6 7 8 9

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Baranski A. et al. Improving the Imaging Contrast of 68Ga-PSMA-11 by Targeted Linker Design: Charged Spacer Moieties Enhance the Pharmacokinetic Properties // Bioconjugate Chemistry. 2017. Vol. 28. No. 9. pp. 2485-2492.

GOST all authors (up to 50) Copy

Baranski A., Schäfer M., Bauder-Wüst U., Wacker A., Schmidt J., Liolios C., Mier W., Haberkorn U., Eisenhut M., Kopka K., Eder M. Improving the Imaging Contrast of 68Ga-PSMA-11 by Targeted Linker Design: Charged Spacer Moieties Enhance the Pharmacokinetic Properties // Bioconjugate Chemistry. 2017. Vol. 28. No. 9. pp. 2485-2492.

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TY - JOUR

DO - 10.1021/acs.bioconjchem.7b00458

UR - https://doi.org/10.1021%2Facs.bioconjchem.7b00458

TI - Improving the Imaging Contrast of 68Ga-PSMA-11 by Targeted Linker Design: Charged Spacer Moieties Enhance the Pharmacokinetic Properties

T2 - Bioconjugate Chemistry

AU - Baranski, Ann-Christin

AU - Schäfer, Martin

AU - Bauder-Wüst, Ulrike

AU - Wacker, Anja

AU - Schmidt, Jana

AU - Haberkorn, Uwe

AU - Eisenhut, Michael

AU - Kopka, Klaus

AU - Mier, Walter

AU - Eder, Matthias

AU - Liolios, Christos

PY - 2017

DA - 2017/08/24 00:00:00

PB - American Chemical Society (ACS)

SP - 2485-2492

IS - 9

VL - 28

SN - 1043-1802

SN - 1520-4812

ER -

BibTex |

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@article{2017_Baranski,

author = {Ann-Christin Baranski and Martin Schäfer and Ulrike Bauder-Wüst and Anja Wacker and Jana Schmidt and Uwe Haberkorn and Michael Eisenhut and Klaus Kopka and Walter Mier and Matthias Eder and Christos Liolios},

title = {Improving the Imaging Contrast of 68Ga-PSMA-11 by Targeted Linker Design: Charged Spacer Moieties Enhance the Pharmacokinetic Properties},

journal = {Bioconjugate Chemistry},

year = {2017},

volume = {28},

publisher = {American Chemical Society (ACS)},

month = {aug},

url = {https://doi.org/10.1021%2Facs.bioconjchem.7b00458},

number = {9},

pages = {2485--2492},

doi = {10.1021/acs.bioconjchem.7b00458}

}

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MLA Copy

Baranski, Ann-Christin, et al. “Improving the Imaging Contrast of 68Ga-PSMA-11 by Targeted Linker Design: Charged Spacer Moieties Enhance the Pharmacokinetic Properties.” Bioconjugate Chemistry, vol. 28, no. 9, Aug. 2017, pp. 2485-2492. https://doi.org/10.1021%2Facs.bioconjchem.7b00458.

Found error?

Publisher

American Chemical Society (ACS)

Journal

Bioconjugate Chemistry

Quartile SCImago

Quartile WOS

Impact factor

4.7

ISSN

10431802 (Print)
15204812 (Electronic)