Development and characterization of a 99m Tc-labeled Neuropeptide Y short analog with potential application in breast cancer imaging
Cardoso, María Elena; Tejería, Emilia; Rey Ríos, Ana María; Terán, Mariella.
Chem Biol Drug Des
; xx: [13 p], 2019.
Artículo
en Inglés
| URUCAN | ID: bcc-5405
The aim of this work was to develop and evaluate a 99m Tc-labeled neuropeptide Y derivative with affinity toward Y1-receptor. The selected amino acid sequence included nine amino acids derived from the C-terminal portion of the NPY complemented with the addition of one cysteine-mercaptoacetic acid moiety to bind the radiometal. Labeling was achieved through the preparation of a 3 + 1 nitrido complex. Physicochemical evaluation, cell uptake, internalization and externalization studies, and competitive assays were performed. Biodistribution experiments were carried out in normal and tumor-bearing mice. A single product with radiochemical purity >90% and high stability was obtained. In vitro analysis showed specific cellular uptake, IC50 of 73.2 nM, and a high internalization rate (80%). Biodistribution studies showed low blood and renal uptake and combined hepatobiliary and urinary elimination. Preliminary studies in mice bearing induced breast tumors rendered promising uptake values(AU)
Biblioteca responsable:
UY78.1
Ubicación: UY78.1 BN-2412
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