Scandium-44: Diagnostic Feasibility in Tumor-Related Angiogenesis

Angiogenesis-related cell-surface molecules, including integrins, aminopeptidase N, vascular endothelial growth factor, and gastrin-releasing peptide receptor (GRPR), play a crucial role in tumour formation. Radiolabelled imaging probes targeting angiogenic biomarkers serve as valuable vectors in tu...

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Main Authors: György Trencsényi, Zita Képes
Format: Article
Language:English
Published: MDPI AG 2023-04-01
Series:International Journal of Molecular Sciences
Subjects:
Online Access:https://www.mdpi.com/1422-0067/24/8/7400
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author György Trencsényi
Zita Képes
author_facet György Trencsényi
Zita Képes
author_sort György Trencsényi
collection DOAJ
description Angiogenesis-related cell-surface molecules, including integrins, aminopeptidase N, vascular endothelial growth factor, and gastrin-releasing peptide receptor (GRPR), play a crucial role in tumour formation. Radiolabelled imaging probes targeting angiogenic biomarkers serve as valuable vectors in tumour identification. Nowadays, there is a growing interest in novel radionuclides other than gallium-68 (<sup>68</sup>Ga) or copper-64 (<sup>64</sup>Cu) to establish selective radiotracers for the imaging of tumour-associated neo-angiogenesis. Given its ideal decay characteristics (E<sub>β</sub><sup>+</sup><sub>average</sub>: 632 KeV) and a half-life (T<sub>1/2</sub> = 3.97 h) that is well matched to the pharmacokinetic profile of small molecules targeting angiogenesis, scandium-44 (<sup>44</sup>Sc) has gained meaningful attention as a promising radiometal for positron emission tomography (PET) imaging. More recently, intensive research has been centered around the investigation of <sup>44</sup>Sc-labelled angiogenesis-directed radiopharmaceuticals. Previous studies dealt with the evaluation of <sup>44</sup>Sc-appended a<sub>v</sub>b<sub>3</sub> integrin–affine Arg-Gly-Asp (RGD) tripeptides, GRPR-selective aminobenzoyl–bombesin analogue (AMBA), and hypoxia-associated nitroimidazole derivatives in the identification of various cancers using experimental tumour models. Given the tumour-related hypoxia- and angiogenesis-targeting capability of these PET probes, <sup>44</sup>Sc seems to be a strong competitor of the currently used positron emitters in radiotracer development. In this review, we summarize the preliminary preclinical achievements with <sup>44</sup>Sc-labelled angiogenesis-specific molecular probes.
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spelling doaj.art-09c8e3c6aefc4a9ea60560361db3521e2023-11-17T19:39:48ZengMDPI AGInternational Journal of Molecular Sciences1661-65961422-00672023-04-01248740010.3390/ijms24087400Scandium-44: Diagnostic Feasibility in Tumor-Related AngiogenesisGyörgy Trencsényi0Zita Képes1Division of Nuclear Medicine and Translational Imaging, Department of Medical Imaging, Faculty of Medicine, University of Debrecen, Nagyerdei St. 98, H-4032 Debrecen, HungaryDivision of Nuclear Medicine and Translational Imaging, Department of Medical Imaging, Faculty of Medicine, University of Debrecen, Nagyerdei St. 98, H-4032 Debrecen, HungaryAngiogenesis-related cell-surface molecules, including integrins, aminopeptidase N, vascular endothelial growth factor, and gastrin-releasing peptide receptor (GRPR), play a crucial role in tumour formation. Radiolabelled imaging probes targeting angiogenic biomarkers serve as valuable vectors in tumour identification. Nowadays, there is a growing interest in novel radionuclides other than gallium-68 (<sup>68</sup>Ga) or copper-64 (<sup>64</sup>Cu) to establish selective radiotracers for the imaging of tumour-associated neo-angiogenesis. Given its ideal decay characteristics (E<sub>β</sub><sup>+</sup><sub>average</sub>: 632 KeV) and a half-life (T<sub>1/2</sub> = 3.97 h) that is well matched to the pharmacokinetic profile of small molecules targeting angiogenesis, scandium-44 (<sup>44</sup>Sc) has gained meaningful attention as a promising radiometal for positron emission tomography (PET) imaging. More recently, intensive research has been centered around the investigation of <sup>44</sup>Sc-labelled angiogenesis-directed radiopharmaceuticals. Previous studies dealt with the evaluation of <sup>44</sup>Sc-appended a<sub>v</sub>b<sub>3</sub> integrin–affine Arg-Gly-Asp (RGD) tripeptides, GRPR-selective aminobenzoyl–bombesin analogue (AMBA), and hypoxia-associated nitroimidazole derivatives in the identification of various cancers using experimental tumour models. Given the tumour-related hypoxia- and angiogenesis-targeting capability of these PET probes, <sup>44</sup>Sc seems to be a strong competitor of the currently used positron emitters in radiotracer development. In this review, we summarize the preliminary preclinical achievements with <sup>44</sup>Sc-labelled angiogenesis-specific molecular probes.https://www.mdpi.com/1422-0067/24/8/7400aminobenzoyl–bombesin analogue (AMBA)aminopeptidase N (APN/CD13)angiogenesiscarcinogenesisgastrin-releasing peptide receptor (GRPR)integrin
spellingShingle György Trencsényi
Zita Képes
Scandium-44: Diagnostic Feasibility in Tumor-Related Angiogenesis
International Journal of Molecular Sciences
aminobenzoyl–bombesin analogue (AMBA)
aminopeptidase N (APN/CD13)
angiogenesis
carcinogenesis
gastrin-releasing peptide receptor (GRPR)
integrin
title Scandium-44: Diagnostic Feasibility in Tumor-Related Angiogenesis
title_full Scandium-44: Diagnostic Feasibility in Tumor-Related Angiogenesis
title_fullStr Scandium-44: Diagnostic Feasibility in Tumor-Related Angiogenesis
title_full_unstemmed Scandium-44: Diagnostic Feasibility in Tumor-Related Angiogenesis
title_short Scandium-44: Diagnostic Feasibility in Tumor-Related Angiogenesis
title_sort scandium 44 diagnostic feasibility in tumor related angiogenesis
topic aminobenzoyl–bombesin analogue (AMBA)
aminopeptidase N (APN/CD13)
angiogenesis
carcinogenesis
gastrin-releasing peptide receptor (GRPR)
integrin
url https://www.mdpi.com/1422-0067/24/8/7400
work_keys_str_mv AT gyorgytrencsenyi scandium44diagnosticfeasibilityintumorrelatedangiogenesis
AT zitakepes scandium44diagnosticfeasibilityintumorrelatedangiogenesis