期刊
NUCLEAR MEDICINE AND BIOLOGY
卷 36, 期 4, 页码 371-378出版社
ELSEVIER SCIENCE INC
DOI: 10.1016/j.nucmedbio.2009.01.005
关键词
c-Met; Glioma; SPECT/CT
c-Met is a receptor tyrosine kinase involved in tumor cell growth, invasion, metastases and angiogenesis. Overexpression of c-Met is frequently observed in several tumor types. Here, we report the in vitro cell-binding properties and biodistribution and SPECT/CT imaging in glioma (U87MG) xenograft-bearing mice of I-125-labeled c-Met-binding peptides (cMBPs) including analogs conjugated to amino acid and aliphatic carbon linkers. In vitro assays showed that the peptide without any linker and those with GGG and 8-aminooctanoic acid linkers had low cellular internalization and that IC50 values of peptides were 1.5 mu M, 65 nM and 85.3 nM, respectively. Biodistribution studies showed the GGG-containing peptide had higher tumor uptake and a higher tumor-to-blood activity concentration ratio than other receptor-binding ligands. SPECT/CT studies with a dedicated small-animal imaging system were performed in U87MG-bearing athymic mice. Although U87MG tumor xenografts could be visualized by SPECT/micro-CT using the various 1251 labeled cMBPs, image contrast and overall quality were unremarkable. (C) 2009 Elsevier Inc. All rights reserved.
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