61Cu-Labelled radiodiagnostics of melanoma with NAPamide-targeted radiopharmaceutical
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Tartalom: http://real.mtak.hu/161324/
Archívum: REAL
Gyűjtemény: Status = Published
Subject = R Medicine / orvostudomány: RM Therapeutics. Pharmacology / terápia, gyógyszertan
Type = Article
Cím:
61Cu-Labelled radiodiagnostics of melanoma with NAPamide-targeted radiopharmaceutical
Létrehozó:
Kálmán-Szabó, Ibolya
Bunda, Szilvia
Lihi, Norbert
Szaniszló, Zsófia
Szikra, Dezső
Péliné Szabó, Judit
Fekete, Anikó
Gyuricza, Barbara
Szücs, Dániel
Papp, Gábor Csaba
Trencsényi, György
Kálmán, Ferenc Krisztián
Dátum:
2023
Téma:
RM Therapeutics. Pharmacology / terápia, gyógyszertan
Tartalmi leírás:
Malignant melanoma is a major public health problem with an increasing incidence and mortality in the Caucasian population due to its significant metastatic potential. The early detection of this cancer type by imaging techniques like positron emission tomography acts as an important contributor to the long-term survival. Based on literature data, the radio labelled alpha-MSH analog NAPamide molecule is an appropriate diagnostic tool for the detection of melanoma tumors. Inspired by these facts, a new radiotracer, the [61Cu]Cu-KFTG-NAPamide has been synthesized to exploit the beneficial features of the positron emitter 61Cu and the melanoma specificity of the NAPamide molecule. In this work, we report a new member of the CB-15aneN5 ligand family (KFTG) as the chelator for 61Cu(II) complexation. On the basis of the thorough physico-chemical characterization, the rigid [Cu(KFTG)]+ complex exhibits fast complex formation (t1/2 = 155 s at pH 5.0 and 25 °C) and high inertness (t1/2 = 2.0 h in 5.0 M HCl at 50 °C) as well as moderate superoxide dismutase activity (IC50 = 2.3 μM). Furthermore, the [61Cu]Cu-KFTG-NAPamide possesses outstanding features in the diagnostics of B16-F10 melanoma tumors by PET imaging: (T/M(SUVs) (in vivo): appr. 14, %ID/g: 7 ± 1 and T/M (ex vivo): 315 ± 24 at 180 min). © 2022 Elsevier B.V.
Nyelv:
angol
Típus:
Article
PeerReviewed
info:eu-repo/semantics/article
Formátum:
text
Azonosító:
Kálmán-Szabó, Ibolya and Bunda, Szilvia and Lihi, Norbert and Szaniszló, Zsófia and Szikra, Dezső and Péliné Szabó, Judit and Fekete, Anikó and Gyuricza, Barbara and Szücs, Dániel and Papp, Gábor Csaba and Trencsényi, György and Kálmán, Ferenc Krisztián (2023) 61Cu-Labelled radiodiagnostics of melanoma with NAPamide-targeted radiopharmaceutical. INTERNATIONAL JOURNAL OF PHARMACEUTICS, 632. ISSN 0378-5173
Kapcsolat:
MTMT:33550899 doi: 10.1016/j.ijpharm.2022.122527