An orally administered multitarget tyrosine kinase inhibitor, SU11248, is a novel potent inhibitor of thyroid oncogenic RET/papillary thyroid cancer kinases.
作者： Dong Wook Kim , Young Suk Jo , Hye Sook Jung , Hyo Kyun Chung , Jung Hun Song
DOI: 10.1210/JC.2005-2845
关键词:
摘要: Context: The oncogenic RET/PTC tyrosine kinase causes papillary thyroid cancer (PTC). use of inhibitors specific for may be useful targeted therapy PTC. Objective: objective the study was to evaluate efficacies recently developed SU11248, SU5416, and SU6668 in inhibition RET/PTC. Design: were synthesized, their inhibitory potencies evaluated using an vitro assay. effects compounds on by quantifying autophosphorylation RET/PTC, signal transducer activator transcription (STAT)-3 activation, morphological reversal RET/PTC-transformed cells. Results: An assay revealed that SU6668, SU11248 inhibited phosphorylation synthetic substrate peptide E4Y RET/PTC3 a dose-dependent manner with IC50 approximately 944 nm 562 224 SU11248. Thus, SU...
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