Journal article

Bivalent Inhibitors of Prostate-Specific Membrane Antigen Conjugated to Desferrioxamine B Squaramide Labeled with Zirconium-89 or Gallium-68 for Diagnostic Imaging of Prostate Cancer

Asif Noor, Jessica K Van Zuylekom, Stacey E Rudd, Kelly Waldeck, Peter D Roselt, Mohammad B Haskali, Michael P Wheatcroft, Eddie Yan, Rodney J Hicks, Carleen Cullinane, Paul S Donnelly

Journal of Medicinal Chemistry | AMER CHEMICAL SOC | Published : 2020


Prostate-specific membrane antigen (PSMA) is a carboxypeptidase that is overexpressed in prostate cancer and is an excellent candidate for targeted diagnostic imaging and therapy. Lysine-ureido-glutamate inhibitors of PSMA radiolabeled with positron-emitting radionuclides can be used for diagnostic imaging with positron emission tomography (PET). A squaramide ester derivative of desferrioxamine B (H3DFOSq) was used to prepare four new agents with either one or two lysine-ureido-glutamate pharmacophores. The H3DFOSq ligand can be used to form stable complexes with either of the positron-emitting radionuclides gallium-68 (t1/2 = 68 min) or zirconium-89 (t1/2 = 3.3 days). The complexes were eva..

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Funding Acknowledgements

The financial support of aspects of this research from Telix Pharmaceuticals is acknowledged. Aspects of the research were supported by the financial support from the National Health and Medical Research Council, Australia (funding to P.S.D., C.C. and P.D.R.). The G8 PET/CT scanner was purchased with the support of a grant from the Australian Cancer Research Foundation. We thank Susan Jackson for expert technical assistance.