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a(SCHEM:ZD6474) -| kin(p(MGI:Ret))
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Approximately 61,000 statements.
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Copyright (c) 2011-2012, Selventa. All rights reserved.
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BEL Framework Large Corpus Document
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1.4
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We recently identified three powerful RET inhibitors: two pyrazolo-pyrimidines: 4-amino-5-(4-methylphenyl)- 7-(t-butyl)pyrazolo[3,4-d]-pyrimidine (PP1) and 4-amino- 5-(4-chloro-phenyl)-7-(t-butyl)pyrazolo[3,4-d]pyrimidine) (PP2), and an anilino- quinazoline: N (4 bromo 2 fluorophenyl) 6 methoxy 7 (1 methylpiperidin 4 yl) methoxy quinazolin 4 amine (ZD6474) [86 88]. These compounds showed half-maximal RET inhibitory concentrations in the nanomolar range (100 nM). When injected into nude mice, fibroblasts transfected with oncogenic RET lost morphological transformation, proliferative autonomy, anchorage-independent growth and tumorigenicity. In addition to inhibition of RET phosphorylation, PP1 induces RET destruction through proteosomal degradation [89].
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Selventa
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2014-07-03T14:30:30.122+02:00
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