Next Article in Journal
Barriers to the Access and Use of Rituximab in Patients with Non-Hodgkin’s Lymphoma and Chronic Lymphocytic Leukemia: A Physician Survey
Next Article in Special Issue
Development and Successful Validation of Simple and Fast TLC Spot Tests for Determination of Kryptofix® 2.2.2 and Tetrabutylammonium in 18F-Labeled Radiopharmaceuticals
Previous Article in Journal
Enhanced Antimicrobial Activity of AamAP1-Lysine, a Novel Synthetic Peptide Analog Derived from the Scorpion Venom Peptide AamAP1
Previous Article in Special Issue
In Vivo Monitoring of the Antiangiogenic Effect of Neurotensin Receptor-Mediated Radiotherapy by Small-Animal Positron Emission Tomography: A Pilot Study
Article Menu

Export Article

Open AccessArticle
Pharmaceuticals 2014, 7(5), 517-529; doi:10.3390/ph7050517

Synthesis, Radiolabelling and In Vitro Characterization of the Gallium-68-, Yttrium-90- and Lutetium-177-Labelled PSMA Ligand, CHX-A''-DTPA-DUPA-Pep

1
Clinic for Nuclear Medicine, University of Ulm, Albert-Einstein-Allee, 89081 Ulm, Germany
2
Department of Health Sciences, University of Milano-Bicocca, Milan 20900, Italy
These authors contributed equally to this work.
*
Author to whom correspondence should be addressed.
Received: 16 December 2013 / Revised: 27 March 2014 / Accepted: 14 April 2014 / Published: 29 April 2014
(This article belongs to the Special Issue Radiopharmaceutical Chemistry between Imaging and Radioendotherapy)
View Full-Text   |   Download PDF [353 KB, uploaded 5 May 2014]   |  

Abstract

Since prostate-specific membrane antigen (PSMA) has been identified as a diagnostic target for prostate cancer, many urea-based small PSMA-targeting molecules were developed. First, the clinical application of these Ga-68 labelled compounds in positron emission tomography (PET) showed their diagnostic potential. Besides, the therapy of prostate cancer is a demanding field, and the use of radiometals with PSMA bearing ligands is a valid approach. In this work, we describe the synthesis of a new PSMA ligand, CHX-A''-DTPA-DUPA-Pep, the subsequent labelling with Ga-68, Lu-177 and Y-90 and the first in vitro characterization. In cell investigations with PSMA-positive LNCaP C4-2 cells, KD values of ≤14.67 ± 1.95 nM were determined, indicating high biological activities towards PSMA. Radiosyntheses with Ga-68, Lu-177 and Y-90 were developed under mild reaction conditions (room temperature, moderate pH of 5.5 and 7.4, respectively) and resulted in nearly quantitative radiochemical yields within 5 min. View Full-Text
Keywords: PSMA; prostate-specific membrane antigen; PET; positron emission tomography; prostate cancer; DUPA; Ga-68; Y-90; Lu-177; radionuclide therapy PSMA; prostate-specific membrane antigen; PET; positron emission tomography; prostate cancer; DUPA; Ga-68; Y-90; Lu-177; radionuclide therapy
Figures

Figure 1

This is an open access article distributed under the Creative Commons Attribution License (CC BY 3.0).

Scifeed alert for new publications

Never miss any articles matching your research from any publisher
  • Get alerts for new papers matching your research
  • Find out the new papers from selected authors
  • Updated daily for 49'000+ journals and 6000+ publishers
  • Define your Scifeed now

SciFeed Share & Cite This Article

MDPI and ACS Style

Baur, B.; Solbach, C.; Andreolli, E.; Winter, G.; Machulla, H.-J.; Reske, S.N. Synthesis, Radiolabelling and In Vitro Characterization of the Gallium-68-, Yttrium-90- and Lutetium-177-Labelled PSMA Ligand, CHX-A''-DTPA-DUPA-Pep. Pharmaceuticals 2014, 7, 517-529.

Show more citation formats Show less citations formats

Related Articles

Article Metrics

Article Access Statistics

1

Comments

[Return to top]
Pharmaceuticals EISSN 1424-8247 Published by MDPI AG, Basel, Switzerland RSS E-Mail Table of Contents Alert
Back to Top