Title : Salinomycin and its derivatives as potent RET transcriptional inhibitors for the treatment of medullary thyroid carcinoma.

Pub. Date : 2020 Jan

PMID : 31746350






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1 Salinomycin and its derivatives as potent RET transcriptional inhibitors for the treatment of medullary thyroid carcinoma. salinomycin ret proto-oncogene Homo sapiens
2 The present study reports the first preclinical characterization of salinomycin and selected analogs as potent RET transcriptional inhibitors. salinomycin ret proto-oncogene Homo sapiens
3 Reverse transcription-PCR and immunoblotting revealed that salinomycin profoundly decreased RET expression in the TT human MTC cell line by inhibiting RET transcription. salinomycin ret proto-oncogene Homo sapiens
4 Reverse transcription-PCR and immunoblotting revealed that salinomycin profoundly decreased RET expression in the TT human MTC cell line by inhibiting RET transcription. salinomycin ret proto-oncogene Homo sapiens
5 Moreover, salinomycin resulted in remarkable anti-proliferative activity against MTC that is driven by RET (gain of function mutation) by selectively inhibiting the intracellular PI3K/Akt/mTOR signaling pathway. salinomycin ret proto-oncogene Homo sapiens
6 Some of the salinomycin derivatives showed the ability to reduce RET expression where others fail to alter RET expression. salinomycin ret proto-oncogene Homo sapiens
7 These results suggest that the RET-suppressing effect of salinomycin may be largely attributed to disruption of the Wnt pathway, presumably through interference with the ternary LRP6-Frizzled-Wnt complex. salinomycin ret proto-oncogene Homo sapiens