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Exploration of peptide T7 and its derivative as integrin αvβ3-targeted imaging agents
OBJECTIVE: The aim of the present study was to develop potential candidates of integrin αvβ3-targeted imaging agent, which can facilitate the diagnosis and treatment of malignant solid tumors. METHODS: Peptides derived from tumstatin, named T7 and T7-6H, were derivatized to contain histidine in the...
Autores principales: | , , , , , |
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Formato: | Online Artículo Texto |
Lenguaje: | English |
Publicado: |
Dove Medical Press
2015
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Materias: | |
Acceso en línea: | https://www.ncbi.nlm.nih.gov/pmc/articles/PMC4474394/ https://www.ncbi.nlm.nih.gov/pubmed/26109872 http://dx.doi.org/10.2147/OTT.S82095 |
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author | He, Xin Hao, Yumei Long, Wei Song, Naling Fan, Saijun Meng, Aimin |
author_facet | He, Xin Hao, Yumei Long, Wei Song, Naling Fan, Saijun Meng, Aimin |
author_sort | He, Xin |
collection | PubMed |
description | OBJECTIVE: The aim of the present study was to develop potential candidates of integrin αvβ3-targeted imaging agent, which can facilitate the diagnosis and treatment of malignant solid tumors. METHODS: Peptides derived from tumstatin, named T7 and T7-6H, were derivatized to contain histidine in the C-terminus of their sequence and were labeled with (99m)Tc via nitrido and carbonyl precursors. The radiochemical purity and stability of (99m)Tc-labeled T7 and T7-6H were characterized by thin-layer chromatography. The whole body biodistribution was studied in NCI-H157-bearing BALB/c nude mice. RESULTS: The (99m)Tc-labeled T7 and T7-6H showed adequate in vitro stability, with a high radiochemical purity of over 90%. The dissociation constant (Kd) value of the (99m)Tc-labeled T7 and T7-6H ranged from 68.5 nM to 140.8 nM in U251 and NCI-H157 cell lines. (99m)Tc-labeled T7 and T7-6H showed no significant difference of biodistribution in mice. Furthermore, both T7 and T7-6H exhibited a poor blood–brain barrier penetration and a transient accumulation in lung; the uptake in tumor tissues was significantly higher than in muscle tissue, with a ratio of 5.8. CONCLUSION: (99m)Tc-labeled T7 and T7-6H can be regarded as promising single-photon emission computed tomography probes for imaging integrin αvβ3, and need to be further studied for noninvasive detection of tumors. |
format | Online Article Text |
id | pubmed-4474394 |
institution | National Center for Biotechnology Information |
language | English |
publishDate | 2015 |
publisher | Dove Medical Press |
record_format | MEDLINE/PubMed |
spelling | pubmed-44743942015-06-24 Exploration of peptide T7 and its derivative as integrin αvβ3-targeted imaging agents He, Xin Hao, Yumei Long, Wei Song, Naling Fan, Saijun Meng, Aimin Onco Targets Ther Original Research OBJECTIVE: The aim of the present study was to develop potential candidates of integrin αvβ3-targeted imaging agent, which can facilitate the diagnosis and treatment of malignant solid tumors. METHODS: Peptides derived from tumstatin, named T7 and T7-6H, were derivatized to contain histidine in the C-terminus of their sequence and were labeled with (99m)Tc via nitrido and carbonyl precursors. The radiochemical purity and stability of (99m)Tc-labeled T7 and T7-6H were characterized by thin-layer chromatography. The whole body biodistribution was studied in NCI-H157-bearing BALB/c nude mice. RESULTS: The (99m)Tc-labeled T7 and T7-6H showed adequate in vitro stability, with a high radiochemical purity of over 90%. The dissociation constant (Kd) value of the (99m)Tc-labeled T7 and T7-6H ranged from 68.5 nM to 140.8 nM in U251 and NCI-H157 cell lines. (99m)Tc-labeled T7 and T7-6H showed no significant difference of biodistribution in mice. Furthermore, both T7 and T7-6H exhibited a poor blood–brain barrier penetration and a transient accumulation in lung; the uptake in tumor tissues was significantly higher than in muscle tissue, with a ratio of 5.8. CONCLUSION: (99m)Tc-labeled T7 and T7-6H can be regarded as promising single-photon emission computed tomography probes for imaging integrin αvβ3, and need to be further studied for noninvasive detection of tumors. Dove Medical Press 2015-06-15 /pmc/articles/PMC4474394/ /pubmed/26109872 http://dx.doi.org/10.2147/OTT.S82095 Text en © 2015 He et al. This work is published by Dove Medical Press Limited, and licensed under Creative Commons Attribution – Non Commercial (unported, v3.0) License The full terms of the License are available at http://creativecommons.org/licenses/by-nc/3.0/. Non-commercial uses of the work are permitted without any further permission from Dove Medical Press Limited, provided the work is properly attributed. |
spellingShingle | Original Research He, Xin Hao, Yumei Long, Wei Song, Naling Fan, Saijun Meng, Aimin Exploration of peptide T7 and its derivative as integrin αvβ3-targeted imaging agents |
title | Exploration of peptide T7 and its derivative as integrin αvβ3-targeted imaging agents |
title_full | Exploration of peptide T7 and its derivative as integrin αvβ3-targeted imaging agents |
title_fullStr | Exploration of peptide T7 and its derivative as integrin αvβ3-targeted imaging agents |
title_full_unstemmed | Exploration of peptide T7 and its derivative as integrin αvβ3-targeted imaging agents |
title_short | Exploration of peptide T7 and its derivative as integrin αvβ3-targeted imaging agents |
title_sort | exploration of peptide t7 and its derivative as integrin αvβ3-targeted imaging agents |
topic | Original Research |
url | https://www.ncbi.nlm.nih.gov/pmc/articles/PMC4474394/ https://www.ncbi.nlm.nih.gov/pubmed/26109872 http://dx.doi.org/10.2147/OTT.S82095 |
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