Radiolabeled NGR-Based Heterodimers for Angiogenesis Imaging: A Review of Preclinical Studies
Since angiogenesis/neoangiogenesis has a major role in tumor development, progression and metastatic spread, the establishment of angiogenesis-targeting imaging and therapeutic vectors is of utmost significance. Aminopeptidase N (APN/CD13) is a pivotal biomarker of angiogenic processes abundantly ex...
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| Format: | Article |
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MDPI AG
2023-09-01
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| Series: | Cancers |
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| Online Access: | https://www.mdpi.com/2072-6694/15/18/4459 |
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| author | György Trencsényi Gábor Halmos Zita Képes |
| author_facet | György Trencsényi Gábor Halmos Zita Képes |
| author_sort | György Trencsényi |
| collection | DOAJ |
| description | Since angiogenesis/neoangiogenesis has a major role in tumor development, progression and metastatic spread, the establishment of angiogenesis-targeting imaging and therapeutic vectors is of utmost significance. Aminopeptidase N (APN/CD13) is a pivotal biomarker of angiogenic processes abundantly expressed on the cell surface of active vascular endothelial and various neoplastic cells, constituting a valuable target for cancer diagnostics and therapy. Since the asparagine–glycine–arginine (NGR) sequence has been shown to colocalize with APN/CD13, the research interest in NGR-peptide-mediated vascular targeting is steadily growing. Earlier preclinical experiments have already demonstrated the imaging and therapeutic feasibility of NGR-based probes labeled with different positron emission tomography (PET) and single-photon emission computed tomography (SPECT) radionuclides, including Gallium-68 (<sup>68</sup>Ga), Copper-64 (<sup>64</sup>Cu), Technetium-99m (<sup>99m</sup>Tc), Lutetium-177 (<sup>177</sup>Lu), Rhenium-188 (<sup>188</sup>Re) or Bismuth-213 (<sup>213</sup>Bi). To improve the tumor binding affinity and the retention time of single-receptor targeting peptides, NGR motifs containing heterodimers have been introduced to identify multi-receptor overexpressing malignancies. Preclinical studies with various tumor-bearing experimental animals provide useful tools for the investigation of the in vivo imaging behavior of NGR-based heterobivalent ligands. Herein, we review the reported preclinical achievements on NGR heterodimers that could be highly relevant for the development of further target-specific multivalent compounds in diagnostic and therapeutic settings. |
| first_indexed | 2024-03-10T22:57:42Z |
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| id | doaj.art-d62c9b6320c5415f866d1223dcfac1f5 |
| institution | Directory Open Access Journal |
| issn | 2072-6694 |
| language | English |
| last_indexed | 2024-03-10T22:57:42Z |
| publishDate | 2023-09-01 |
| publisher | MDPI AG |
| record_format | Article |
| series | Cancers |
| spelling | doaj.art-d62c9b6320c5415f866d1223dcfac1f52023-11-19T09:54:05ZengMDPI AGCancers2072-66942023-09-011518445910.3390/cancers15184459Radiolabeled NGR-Based Heterodimers for Angiogenesis Imaging: A Review of Preclinical StudiesGyörgy Trencsényi0Gábor Halmos1Zita Képes2Division of Nuclear Medicine and Translational Imaging, Department of Medical Imaging, Faculty of Medicine, University of Debrecen, Nagyerdei St. 98, H-4032 Debrecen, HungaryDepartment of Biopharmacy, Faculty of Pharmacy, 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, HungarySince angiogenesis/neoangiogenesis has a major role in tumor development, progression and metastatic spread, the establishment of angiogenesis-targeting imaging and therapeutic vectors is of utmost significance. Aminopeptidase N (APN/CD13) is a pivotal biomarker of angiogenic processes abundantly expressed on the cell surface of active vascular endothelial and various neoplastic cells, constituting a valuable target for cancer diagnostics and therapy. Since the asparagine–glycine–arginine (NGR) sequence has been shown to colocalize with APN/CD13, the research interest in NGR-peptide-mediated vascular targeting is steadily growing. Earlier preclinical experiments have already demonstrated the imaging and therapeutic feasibility of NGR-based probes labeled with different positron emission tomography (PET) and single-photon emission computed tomography (SPECT) radionuclides, including Gallium-68 (<sup>68</sup>Ga), Copper-64 (<sup>64</sup>Cu), Technetium-99m (<sup>99m</sup>Tc), Lutetium-177 (<sup>177</sup>Lu), Rhenium-188 (<sup>188</sup>Re) or Bismuth-213 (<sup>213</sup>Bi). To improve the tumor binding affinity and the retention time of single-receptor targeting peptides, NGR motifs containing heterodimers have been introduced to identify multi-receptor overexpressing malignancies. Preclinical studies with various tumor-bearing experimental animals provide useful tools for the investigation of the in vivo imaging behavior of NGR-based heterobivalent ligands. Herein, we review the reported preclinical achievements on NGR heterodimers that could be highly relevant for the development of further target-specific multivalent compounds in diagnostic and therapeutic settings.https://www.mdpi.com/2072-6694/15/18/4459Aminopeptidase N (APN/CD13)angiogenesisasparagine–glycine–arginine (NGR)heterodimerpreclinicalradiolabeled |
| spellingShingle | György Trencsényi Gábor Halmos Zita Képes Radiolabeled NGR-Based Heterodimers for Angiogenesis Imaging: A Review of Preclinical Studies Cancers Aminopeptidase N (APN/CD13) angiogenesis asparagine–glycine–arginine (NGR) heterodimer preclinical radiolabeled |
| title | Radiolabeled NGR-Based Heterodimers for Angiogenesis Imaging: A Review of Preclinical Studies |
| title_full | Radiolabeled NGR-Based Heterodimers for Angiogenesis Imaging: A Review of Preclinical Studies |
| title_fullStr | Radiolabeled NGR-Based Heterodimers for Angiogenesis Imaging: A Review of Preclinical Studies |
| title_full_unstemmed | Radiolabeled NGR-Based Heterodimers for Angiogenesis Imaging: A Review of Preclinical Studies |
| title_short | Radiolabeled NGR-Based Heterodimers for Angiogenesis Imaging: A Review of Preclinical Studies |
| title_sort | radiolabeled ngr based heterodimers for angiogenesis imaging a review of preclinical studies |
| topic | Aminopeptidase N (APN/CD13) angiogenesis asparagine–glycine–arginine (NGR) heterodimer preclinical radiolabeled |
| url | https://www.mdpi.com/2072-6694/15/18/4459 |
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