Design and synthesis of a new conjugate of a tris(3-hydroxy-4-pyridinone) chelator (KC18) for potential use as gallium-68-labeled prostate-specific membrane antigen (PSMA) radiopharmaceutical

Prostate-specific membrane antigen (PSMA) is considered a significant target for the diagnosis and therapy of prostate cancer. 2-[3-(1,3-dicarboxypropyl)-ureido]pentanedioic acid (DUPA) is a promising binding motif that has been proved to target PSMA successfully. 3-Hydroxy-4-pyridinone units contai...

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Main Authors:	Xu Zhou, Lin-Lin Dong, Yuying Li, Meng-Chao Cui, Lang-Tao Shen
Format:	article
Language:	EN
Published:	Elsevier 2021
Subjects:	Prostate specific membrane antigen (PSMA) Tris(3-hydroxy-4-pyridinone) 2-[3-(1,3-dicarboxypropyl)-ureido]pentanedioic acid (DUPA) Positron emission tomography (PET) Radiopharmaceutical Chemistry QD1-999
Online Access:	https://doaj.org/article/7b690681e2df43a3ae95e7c4bfe5b383
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spelling	oai:doaj.org-article:7b690681e2df43a3ae95e7c4bfe5b3832021-11-12T04:32:30ZDesign and synthesis of a new conjugate of a tris(3-hydroxy-4-pyridinone) chelator (KC18) for potential use as gallium-68-labeled prostate-specific membrane antigen (PSMA) radiopharmaceutical2211-715610.1016/j.rechem.2021.100240https://doaj.org/article/7b690681e2df43a3ae95e7c4bfe5b3832021-01-01T00:00:00Zhttp://www.sciencedirect.com/science/article/pii/S2211715621001454https://doaj.org/toc/2211-7156Prostate-specific membrane antigen (PSMA) is considered a significant target for the diagnosis and therapy of prostate cancer. 2-[3-(1,3-dicarboxypropyl)-ureido]pentanedioic acid (DUPA) is a promising binding motif that has been proved to target PSMA successfully. 3-Hydroxy-4-pyridinone units containing multidentate bifunctional chelators could chelate gallium(III) at mild conditions effectively. In this letter, we combine DUPA with a tris(hydroxypyridinone) bifunctional chelator and get a novel precursor of gallium-68 radiopharmaceutical, DUPA-β-Ala-KC18. The synthesis, characterization of DUPA-β-Ala-KC18 and the formation of its natural-abundance gallium(III) complex are presented. DUPA-β-Ala-KC18 displayed a binding affinity to PSMA.Xu ZhouLin-Lin DongYuying LiMeng-Chao CuiLang-Tao ShenElsevierarticleProstate specific membrane antigen (PSMA)Tris(3-hydroxy-4-pyridinone)2-[3-(1,3-dicarboxypropyl)-ureido]pentanedioic acid (DUPA)Positron emission tomography (PET)RadiopharmaceuticalChemistryQD1-999ENResults in Chemistry, Vol 3, Iss , Pp 100240- (2021)
institution	DOAJ
collection	DOAJ
language	EN
topic	Prostate specific membrane antigen (PSMA) Tris(3-hydroxy-4-pyridinone) 2-[3-(1,3-dicarboxypropyl)-ureido]pentanedioic acid (DUPA) Positron emission tomography (PET) Radiopharmaceutical Chemistry QD1-999
spellingShingle	Prostate specific membrane antigen (PSMA) Tris(3-hydroxy-4-pyridinone) 2-[3-(1,3-dicarboxypropyl)-ureido]pentanedioic acid (DUPA) Positron emission tomography (PET) Radiopharmaceutical Chemistry QD1-999 Xu Zhou Lin-Lin Dong Yuying Li Meng-Chao Cui Lang-Tao Shen Design and synthesis of a new conjugate of a tris(3-hydroxy-4-pyridinone) chelator (KC18) for potential use as gallium-68-labeled prostate-specific membrane antigen (PSMA) radiopharmaceutical
description	Prostate-specific membrane antigen (PSMA) is considered a significant target for the diagnosis and therapy of prostate cancer. 2-[3-(1,3-dicarboxypropyl)-ureido]pentanedioic acid (DUPA) is a promising binding motif that has been proved to target PSMA successfully. 3-Hydroxy-4-pyridinone units containing multidentate bifunctional chelators could chelate gallium(III) at mild conditions effectively. In this letter, we combine DUPA with a tris(hydroxypyridinone) bifunctional chelator and get a novel precursor of gallium-68 radiopharmaceutical, DUPA-β-Ala-KC18. The synthesis, characterization of DUPA-β-Ala-KC18 and the formation of its natural-abundance gallium(III) complex are presented. DUPA-β-Ala-KC18 displayed a binding affinity to PSMA.
format	article
author	Xu Zhou Lin-Lin Dong Yuying Li Meng-Chao Cui Lang-Tao Shen
author_facet	Xu Zhou Lin-Lin Dong Yuying Li Meng-Chao Cui Lang-Tao Shen
author_sort	Xu Zhou
title	Design and synthesis of a new conjugate of a tris(3-hydroxy-4-pyridinone) chelator (KC18) for potential use as gallium-68-labeled prostate-specific membrane antigen (PSMA) radiopharmaceutical
title_short	Design and synthesis of a new conjugate of a tris(3-hydroxy-4-pyridinone) chelator (KC18) for potential use as gallium-68-labeled prostate-specific membrane antigen (PSMA) radiopharmaceutical
title_full	Design and synthesis of a new conjugate of a tris(3-hydroxy-4-pyridinone) chelator (KC18) for potential use as gallium-68-labeled prostate-specific membrane antigen (PSMA) radiopharmaceutical
title_fullStr	Design and synthesis of a new conjugate of a tris(3-hydroxy-4-pyridinone) chelator (KC18) for potential use as gallium-68-labeled prostate-specific membrane antigen (PSMA) radiopharmaceutical
title_full_unstemmed	Design and synthesis of a new conjugate of a tris(3-hydroxy-4-pyridinone) chelator (KC18) for potential use as gallium-68-labeled prostate-specific membrane antigen (PSMA) radiopharmaceutical
title_sort	design and synthesis of a new conjugate of a tris(3-hydroxy-4-pyridinone) chelator (kc18) for potential use as gallium-68-labeled prostate-specific membrane antigen (psma) radiopharmaceutical
publisher	Elsevier
publishDate	2021
url	https://doaj.org/article/7b690681e2df43a3ae95e7c4bfe5b383
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Design and synthesis of a new conjugate of a tris(3-hydroxy-4-pyridinone) chelator (KC18) for potential use as gallium-68-labeled prostate-specific membrane antigen (PSMA) radiopharmaceutical

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