Diagnosis of Melanoma with 61Cu-Labeled PET Tracer

Bunda, Szilvia and Kálmán-Szabó, Ibolya and Lihi, Norbert and Képes, Zita and Szikra, Dezső and Péliné Szabó, Judit and Timári, István and Szücs, Dániel and May, Nóra Veronika and Papp, Gábor Csaba and Trencsényi, György and Kálmán, Ferenc Krisztián (2024) Diagnosis of Melanoma with 61Cu-Labeled PET Tracer. JOURNAL OF MEDICINAL CHEMISTRY, 67, (11). pp. 9342-9354. ISSN 0022-2623

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Official URL: https://doi.org/10.1021/acs.jmedchem.4c00479

Abstract

Until the recent years, substances containing radioactive Cu-61 were strongly considered as potential positron-emitting radiopharmaceuticals for use in positron emission tomography (PET) applications; however, due to their suitably long half-life, and generator-independent and cost-effective production, they seem to be economically viable for human imaging. Since malignant melanoma (MM) is a major public health problem, its early diagnosis is a crucial contributor to long-term survival, which can be achieved using radiolabeled alpha-melanocyte-stimulating hormone analog NAPamide derivatives. Here, we report on the physicochemical features of a new CB-15aneN(5)-based Cu(II) complex ([Cu(KFTGdiac)](-)) and the ex vivo and in vivo characterization of its NAPamide conjugate. The rigid chelate possesses prompt complex formation and suitable inertness (t(1/2) = 18.4 min in 5.0 M HCl at 50 degrees C), as well as excellent features in the diagnosis of B16-F10 melanoma tumors (T/M(SUVs) (in vivo): 12.7, %ID/g: 6.6 +/- 0.3, T/M (ex vivo): 22).

Item Type:	Article
Additional Information:	Funding Agency and Grant Number: Magyar Tudom?nyos Akad?mia [FK-134551]; Hungarian National Research, Development and Innovation Office [UNKP-23-5, UNKP-23-4-II]; New National Excellence Program; National Research, Development and Innovation Fund; Janos Bolyai Research Scholarship of the Hungarian Academy of Sciences; Ministry for Innovation and Technology from the source of the National Research, Development and Innovation Fund; University of Debrecen Scientific Research Bridging Fund Funding text: The research was funded by the Hungarian National Research, Development and Innovation Office (FK-134551) project, the New National Excellence Program UNKP-23-5, and the UNKP-23-4-II New National Excellence Program of The Ministry for Culture and Innovation from the source of the National Research, Development and Innovation Fund (K.Z.). F.K.K. and N.L. acknowledge the financial support of the Janos Bolyai Research Scholarship of the Hungarian Academy of Sciences. The authors are indebted to KIFU for awarding access to the resources based in Hungary. The research was supported by the KDP-2021 program of the Ministry for Innovation and Technology from the source of the National Research, Development and Innovation Fund (G.T. and I.K.-S.). This work is also supported by the University of Debrecen Scientific Research Bridging Fund (DETKA).
Uncontrolled Keywords:	PEPTIDES; COMPLEXATION; ANALOGS;
Subjects:	R Medicine / orvostudomány > R1 Medicine (General) / orvostudomány általában > R850-854 Experimental medicine / kisérleti orvostudomány
SWORD Depositor:	MTMT SWORD
Depositing User:	MTMT SWORD
Date Deposited:	23 Sep 2024 06:37
Last Modified:	23 Sep 2024 06:37
URI:	https://real.mtak.hu/id/eprint/205509

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