Efficient inhibition of RET/papillary thyroid carcinoma oncogenic kinases by 4-amino-5-(4-chloro-phenyl)-7-(t-butyl)pyrazolo[3,4-d]pyrimidine (PP2).

@article{Carlomagno2003EfficientIO,
  title={Efficient inhibition of RET/papillary thyroid carcinoma oncogenic kinases by 4-amino-5-(4-chloro-phenyl)-7-(t-butyl)pyrazolo[3,4-d]pyrimidine (PP2).},
  author={Francesca Carlomagno and Donata Vitagliano and Teresa Guida and Fulvio Basolo and Maria Domenica Castellone and Rosa Marina Melillo and Alfredo Fusco and Massimo Santoro},
  journal={The Journal of clinical endocrinology and metabolism},
  year={2003},
  volume={88 4},
  pages={1897-902}
}
Inappropriate activation of the RET receptor tyrosine kinase causes development of papillary and medullary thyroid cancer. We have previously shown that pyrazolopyrimidine is a potent inhibitor of the RET kinase. Here, we show that 4-amino-5-(4-chloro-phenyl)-7-(t-butyl)pyrazolo[3,4-d]pyrimidine) (PP2), another pyrazolopyrimidine, blocks the enzymatic activity of the isolated RET kinase and RET/PTC1 oncoprotein at IC(50) in the nanomolar range. PP2 blocked in vivo phosphorylation and signaling… CONTINUE READING
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