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- W199756487 abstract "1953 Objectives Kinase blockade is an effective therapeutic strategy in the clinic. However, non-invasive methods to discern which patients bear the target (and therefore presumably are more likely to respond) remain a critical challenge. This study was aimed to radiosynthesize 111In-labeled phosphotyrosine antibody for assessment of epidermal growth factor receptor (EGFR) tyrosine phosphorylation activity. Methods We labeled an anti-phosphotyrosine antibody with indium (111In) using ethylenedicysteine (EC) as a chelator (111In-EC-P-Tyr). We hypothesized that tumor phosphokinase activity would be discernible by in vivo planar imaging with the use of 111In-EC-P-Tyr. A xenograft (A431) expressing amplified EGFR was used as a model, with H441 (wild-type EGFR) xenografts as a control. Results 111In-EC-P-Tyr successfully imaged A431 tumor xenografts. After the mice ingested the EGFR inhibitor gefitinib for three consecutive days, tumor uptake changes in the A431 model could be imaged by 111In-EC-P-Tyr, but not in the H441 model. Biodistribution studies confirmed tumor uptake of 111In-EC-P-Tyr. Conclusions Our results inidcate that 111In-EC-P-Tyr is a novel imaging agent that can assess tumor phosphotyrosine kinase activity in animal models. Such an agent merits investigation in the clinic to determine if it can detect early evidence of changes in phosphotyrosine kinase levels after treatment with a kinase inhibitor." @default.
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- W199756487 date "2009-05-01" @default.
- W199756487 modified "2023-09-28" @default.
- W199756487 title "Assessment of EGFR tyrosine phosphorylation using 111In-EC-antiphosphotyrosine monoclonal antibody in animal models" @default.
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