[<sup>99m</sup>Tc]Tc-Labeled Plectin-Targeting Peptide as a Novel SPECT Probe for Tumor Imaging
Certain receptors are often overexpressed during tumor occurrence and development and closely correlate with carcinogenesis. Owing to its overexpression on the cell membrane and cytoplasm of various tumors, plectin, which is involved in tumor proliferation, migration, and invasion, has been viewed a...
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MDPI AG
2022-05-01
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| Series: | Pharmaceutics |
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| Online Access: | https://www.mdpi.com/1999-4923/14/5/996 |
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| author | Jiali Gong Lingzhou Zhao Jiqin Yang Meilin Zhu Jinhua Zhao |
| author_facet | Jiali Gong Lingzhou Zhao Jiqin Yang Meilin Zhu Jinhua Zhao |
| author_sort | Jiali Gong |
| collection | DOAJ |
| description | Certain receptors are often overexpressed during tumor occurrence and development and closely correlate with carcinogenesis. Owing to its overexpression on the cell membrane and cytoplasm of various tumors, plectin, which is involved in tumor proliferation, migration, and invasion, has been viewed as a promising target for cancer imaging. Hence, plectin-targeting agents have great potential as imaging probes for tumor diagnosis. In this study, we developed a [<sup>99m</sup>Tc]Tc-labeled plectin-targeted peptide (PTP) as a novel single-photon emission computed tomography (SPECT) probe for tumor imaging and investigated its pharmacokinetics, biodistribution, and targeting ability in several types of tumor-bearing mouse models. The PTP had good biocompatibility and targeting ability to tumor cells in vitro and could be readily labeled with [<sup>99m</sup>Tc]Tc after modification with the bifunctional chelator 6-hydrazino nicotinamide (HYNIC). Furthermore, the prepared [<sup>99m</sup>Tc]Tc-labeled PTP ([<sup>99m</sup>Tc]Tc-HYNIC-PTP) showed high radiochemical purity and excellent stability in vitro. In addition, favorable biodistribution, fast blood clearance, and clear accumulation of [<sup>99m</sup>Tc]Tc-HYNIC-PTP in several types of tumors were observed, with a good correlation between tumor uptake and plectin expression levels. These results indicate the potential of [<sup>99m</sup>Tc]Tc-HYNIC-PTP as a novel SPECT probe for tumor imaging. |
| first_indexed | 2024-03-10T03:07:31Z |
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| id | doaj.art-616576c1aefd415fb3b492f658da9c82 |
| institution | Directory Open Access Journal |
| issn | 1999-4923 |
| language | English |
| last_indexed | 2024-03-10T03:07:31Z |
| publishDate | 2022-05-01 |
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| series | Pharmaceutics |
| spelling | doaj.art-616576c1aefd415fb3b492f658da9c822023-11-23T12:37:50ZengMDPI AGPharmaceutics1999-49232022-05-0114599610.3390/pharmaceutics14050996[<sup>99m</sup>Tc]Tc-Labeled Plectin-Targeting Peptide as a Novel SPECT Probe for Tumor ImagingJiali Gong0Lingzhou Zhao1Jiqin Yang2Meilin Zhu3Jinhua Zhao4Department of Nuclear Medicine, Shanghai General Hospital, Shanghai Jiao Tong University School of Medicine, Shanghai 200080, ChinaDepartment of Nuclear Medicine, Shanghai General Hospital, Shanghai Jiao Tong University School of Medicine, Shanghai 200080, ChinaDepartment of Nuclear Medicine, General Hospital of Ningxia Medical University, Yinchuan 750004, ChinaSchool of Basic Medical Sciences, Ningxia Medical University, Yinchuan 750004, ChinaDepartment of Nuclear Medicine, Shanghai General Hospital, Shanghai Jiao Tong University School of Medicine, Shanghai 200080, ChinaCertain receptors are often overexpressed during tumor occurrence and development and closely correlate with carcinogenesis. Owing to its overexpression on the cell membrane and cytoplasm of various tumors, plectin, which is involved in tumor proliferation, migration, and invasion, has been viewed as a promising target for cancer imaging. Hence, plectin-targeting agents have great potential as imaging probes for tumor diagnosis. In this study, we developed a [<sup>99m</sup>Tc]Tc-labeled plectin-targeted peptide (PTP) as a novel single-photon emission computed tomography (SPECT) probe for tumor imaging and investigated its pharmacokinetics, biodistribution, and targeting ability in several types of tumor-bearing mouse models. The PTP had good biocompatibility and targeting ability to tumor cells in vitro and could be readily labeled with [<sup>99m</sup>Tc]Tc after modification with the bifunctional chelator 6-hydrazino nicotinamide (HYNIC). Furthermore, the prepared [<sup>99m</sup>Tc]Tc-labeled PTP ([<sup>99m</sup>Tc]Tc-HYNIC-PTP) showed high radiochemical purity and excellent stability in vitro. In addition, favorable biodistribution, fast blood clearance, and clear accumulation of [<sup>99m</sup>Tc]Tc-HYNIC-PTP in several types of tumors were observed, with a good correlation between tumor uptake and plectin expression levels. These results indicate the potential of [<sup>99m</sup>Tc]Tc-HYNIC-PTP as a novel SPECT probe for tumor imaging.https://www.mdpi.com/1999-4923/14/5/996plectinplectin-targeting peptide[<sup>99m</sup>Tc]Tctumor imaging |
| spellingShingle | Jiali Gong Lingzhou Zhao Jiqin Yang Meilin Zhu Jinhua Zhao [<sup>99m</sup>Tc]Tc-Labeled Plectin-Targeting Peptide as a Novel SPECT Probe for Tumor Imaging Pharmaceutics plectin plectin-targeting peptide [<sup>99m</sup>Tc]Tc tumor imaging |
| title | [<sup>99m</sup>Tc]Tc-Labeled Plectin-Targeting Peptide as a Novel SPECT Probe for Tumor Imaging |
| title_full | [<sup>99m</sup>Tc]Tc-Labeled Plectin-Targeting Peptide as a Novel SPECT Probe for Tumor Imaging |
| title_fullStr | [<sup>99m</sup>Tc]Tc-Labeled Plectin-Targeting Peptide as a Novel SPECT Probe for Tumor Imaging |
| title_full_unstemmed | [<sup>99m</sup>Tc]Tc-Labeled Plectin-Targeting Peptide as a Novel SPECT Probe for Tumor Imaging |
| title_short | [<sup>99m</sup>Tc]Tc-Labeled Plectin-Targeting Peptide as a Novel SPECT Probe for Tumor Imaging |
| title_sort | sup 99m sup tc tc labeled plectin targeting peptide as a novel spect probe for tumor imaging |
| topic | plectin plectin-targeting peptide [<sup>99m</sup>Tc]Tc tumor imaging |
| url | https://www.mdpi.com/1999-4923/14/5/996 |
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