Article
CEP-701 and CEP-751 inhibit constitutively activated RET tyrosine kinase activity and block medullary thyroid carcinoma cell growth.
Cancer research - 1 Sept 2003
Strock Christopher J, Park Jong-In, Rosen Mark, Dionne Craig, Ruggeri Bruce, Jones-Bolin Susan, Denmeade Samuel R, Ball Douglas W, Nelkin Barry D
Abstract excerpt
All of the cases of medullary thyroid carcinoma (MTC) express the RET receptor tyrosine kinase. In essentially all of the hereditary cases and approximately 40% of the sporadic cases of MTC, the RET kinase is constitutively activated by mutation. This suggests that RET may be an effective therapeutic target for treatment of MTC. We show that the indolocarbazole derivatives, CEP-701 and CEP-751, inhibit RET in MTC...
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