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
| Autor: | Lin-Lin Dong, Lang-Tao Shen, Xu Zhou, Yuying Li, Meng-Chao Cui |
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| Rok vydání: | 2021 |
| Předmět: |
Tris
Tris(3-hydroxy-4-pyridinone) Denticity 2-[3-(1 3-dicarboxypropyl)-ureido]pentanedioic acid (DUPA) chemistry.chemical_element General Chemistry Combinatorial chemistry Chemistry chemistry.chemical_compound Prostate specific membrane antigen (PSMA) chemistry Positron emission tomography (PET) Glutamate carboxypeptidase II Radiopharmaceutical Chelation Bifunctional chelator Gallium Bifunctional QD1-999 Conjugate |
| Zdroj: | Results in Chemistry, Vol 3, Iss, Pp 100240-(2021) |
| ISSN: | 2211-7156 |
| Popis: | 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. |
| Databáze: | OpenAIRE |
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