ArticleOncoTargets and therapy2015
Exploration of peptide T7 and its derivative as integrin αvβ3-targeted imaging agents.
Article in OncoTargets and therapy, 2015. The graph could read no effect estimate from its abstract, so it casts no vote on the map. Cited by 3 papers.
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Who cites it
3 citing papers in PubMed, 5 citations in OpenAlex.
- Bone sialoprotein stimulates cancer cell adhesion through the RGD motif and the αvβ3 and αvβ5 integrin receptors.Oncology letters · 2024Article
- Assessment of bioactive peptides derived from laminin-111 as prospective breast cancer-targeting agents.Amino acids · 2024Article
- Matricryptins Network with Matricellular Receptors at the Surface of Endothelial and Tumor Cells.Frontiers in pharmacology · 2016Review
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Authors and funding
6 authors at 1 institution in 1 country.
Funding
No grant is acknowledged in the PubMed record.
Abstract
objectiveThe 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.
methodsPeptides 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.
resultsThe (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.
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