Title |
Exploration of peptide T7 and its derivative as integrin αvβ3-targeted imaging agents
|
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Published in |
OncoTargets and therapy, June 2015
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DOI | 10.2147/ott.s82095 |
Pubmed ID | |
Authors |
Xin He, Yumei Hao, Wei Long, Naling Song, Saijun Fan, Aimin Meng |
Abstract |
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. 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. 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. (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. |
Mendeley readers
Geographical breakdown
Country | Count | As % |
---|---|---|
Unknown | 13 | 100% |
Demographic breakdown
Readers by professional status | Count | As % |
---|---|---|
Student > Ph. D. Student | 2 | 15% |
Student > Bachelor | 2 | 15% |
Professor > Associate Professor | 1 | 8% |
Student > Postgraduate | 1 | 8% |
Unknown | 7 | 54% |
Readers by discipline | Count | As % |
---|---|---|
Pharmacology, Toxicology and Pharmaceutical Science | 2 | 15% |
Chemical Engineering | 1 | 8% |
Mathematics | 1 | 8% |
Agricultural and Biological Sciences | 1 | 8% |
Medicine and Dentistry | 1 | 8% |
Other | 0 | 0% |
Unknown | 7 | 54% |