There is no effective treatment for recurrent or metastatic medullary thyroid carcinoma (MTC), a tumor arising from thyroid C-cells commonly presenting an inherited or acquired RET mutation. In this study we examined the sensitivity of two human MTC cell lines to novel pyrazolopyrimidine derivates, able to inhibit src-family tyrosine kinase activity. In TT cells [carrying the multiple endocrine neoplasia (MEN)2A Ret mutation Cys 634Trp] and MZ-CRC-1 cells (carrying the MEN2B RET mutation Met891Thr), one of these compounds, namely Si 34, determined a significant growth inhibitory effect (approximately 90% vs control for TT, 80% vs control for MZ-CRC-1) mainly due to enhanced cell mortality after a 6-day incubation. At concentrations that increased cell mortality, neither biochemical or morphological characteristics of apoptosis were detected in TT and MZCRC- 1 cells treated with Si 34. These results, when confirmed in other in vivo preclinical models, suggest that this novel tyrosine kinase inhibitor may be useful for the treatment of MTC.
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|Titolo:||Growth inhibition of medullary thyroid carcinoma cells by pyrazolo-pyrimidine derivatives|
|Rivista:||JOURNAL OF ENDOCRINOLOGICAL INVESTIGATION|
|Citazione:||R., M., M., C., E., T., S., S., M., N., E., F., et al. (2007). Growth inhibition of medullary thyroid carcinoma cells by pyrazolo-pyrimidine derivatives. JOURNAL OF ENDOCRINOLOGICAL INVESTIGATION, 30(10), 31-34.|
|Appare nelle tipologie:||1.1 Articolo in rivista|
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