作者
Dong Wook Kim, Young Suk Jo, Hye Sook Jung, Hyo Kyun Chung, Jung Hun Song, Ki Cheol Park, Su Hyeon Park, Jung Hwan Hwang, So Young Rha, Gi Ryang Kweon, Su-Jae Lee, Ki-Won Jo, Minho Shong
发表日期
2006/10/1
期刊
The Journal of Clinical Endocrinology & Metabolism
卷号
91
期号
10
页码范围
4070-4076
出版商
Oxford University Press
简介
Context: The oncogenic RET/PTC tyrosine kinase causes papillary thyroid cancer (PTC). The use of inhibitors specific for RET/PTC may be useful for targeted therapy of PTC.
Objective: The objective of the study was to evaluate the efficacies of the recently developed kinase inhibitors SU11248, SU5416, and SU6668 in inhibition of RET/PTC.
Design: SU11248, SU5416, and SU6668 were synthesized, and their inhibitory potencies were evaluated using an in vitro RET/PTC kinase assay. The inhibitory effects of the compounds on RET/PTC were evaluated by quantifying the autophosphorylation of RET/PTC, signal transducer and activator of transcription (STAT)-3 activation, and the morphological reversal of RET/PTC-transformed cells.
Results: An in vitro kinase assay revealed that SU5416, SU6668, and SU11248 inhibited phosphorylation of the synthetic tyrosine kinase …
引用总数
学术搜索中的文章
DW Kim, YS Jo, HS Jung, HK Chung, JH Song… - The Journal of Clinical Endocrinology & Metabolism, 2006