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
1
,
Jessica van Zuylekom
2
,
Stacey E. Rudd
1
,
Kelly Waldeck
2
,
Peter Roselt
2
,
Mohammad B. Haskali
2
,
Michael P. Wheatcroft
3
,
Eddie Yan
3
,
Rodney J. Hicks
2, 4
,
Carleen Cullinane
2, 4
,
3
Telix Pharmaceuticals Limited, Suite 401, 55 Flemington Road, North Melbourne, Victoria 3051, Australia
|
Publication type: Journal Article
Publication date: 2020-07-29
scimago Q1
wos Q1
SJR: 1.801
CiteScore: 11.5
Impact factor: 6.8
ISSN: 00222623, 15204804
PubMed ID:
32786229
Drug Discovery
Molecular Medicine
Abstract
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 evaluated in PSMA-positive xenograft mouse models. Bivalent inhibitors, where two pharmacophores are tethered to a single DFOSq ligand, have better tumor uptake than their monovalent analogues. The ligands presented here, which can be labeled with either gallium-68 or zirconium-89, have the potential to increase the number of clinical sites that can perform diagnostic PET imaging.
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Total citations:
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GOST
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Noor A. et al. 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 // Journal of Medicinal Chemistry. 2020. Vol. 63. No. 17. pp. 9258-9270.
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Noor A., van Zuylekom J., Rudd S. E., Waldeck K., Roselt P., Haskali M. B., Wheatcroft M. P., Yan E., Hicks R. J., Cullinane C., Donnelly P. S. 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 // Journal of Medicinal Chemistry. 2020. Vol. 63. No. 17. pp. 9258-9270.
Cite this
RIS
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TY - JOUR
DO - 10.1021/acs.jmedchem.0c00291
UR - https://doi.org/10.1021/acs.jmedchem.0c00291
TI - 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
T2 - Journal of Medicinal Chemistry
AU - Noor, Asif
AU - van Zuylekom, Jessica
AU - Rudd, Stacey E.
AU - Waldeck, Kelly
AU - Roselt, Peter
AU - Haskali, Mohammad B.
AU - Wheatcroft, Michael P.
AU - Yan, Eddie
AU - Hicks, Rodney J.
AU - Cullinane, Carleen
AU - Donnelly, Paul S.
PY - 2020
DA - 2020/07/29
PB - American Chemical Society (ACS)
SP - 9258-9270
IS - 17
VL - 63
PMID - 32786229
SN - 0022-2623
SN - 1520-4804
ER -
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BibTex (up to 50 authors)
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@article{2020_Noor,
author = {Asif Noor and Jessica van Zuylekom and Stacey E. Rudd and Kelly Waldeck and Peter Roselt and Mohammad B. Haskali and Michael P. Wheatcroft and Eddie Yan and Rodney J. Hicks and Carleen Cullinane and Paul S. Donnelly},
title = {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},
journal = {Journal of Medicinal Chemistry},
year = {2020},
volume = {63},
publisher = {American Chemical Society (ACS)},
month = {jul},
url = {https://doi.org/10.1021/acs.jmedchem.0c00291},
number = {17},
pages = {9258--9270},
doi = {10.1021/acs.jmedchem.0c00291}
}
Cite this
MLA
Copy
Noor, Asif, et al. “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.” Journal of Medicinal Chemistry, vol. 63, no. 17, Jul. 2020, pp. 9258-9270. https://doi.org/10.1021/acs.jmedchem.0c00291.
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