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    11ms
    Therapeutic strategy using novel RET/YES1 dual-target inhibitor in lung cancer. (PubMed, Biomed Pharmacother)
    In this study, we investigated PLM-101, a novel dual-target inhibitor of RET/YES1, which exhibits notable anti-cancer activities against CCDC6-RET-positive cancer cells and anti-metastatic effects against YES1-positive cancer cells. Our findings shed light on the significance of the YES1-Cortactin-actin remodeling pathway in the metastasis of lung cancer cells, establishing YES1 as a promising target for suppression of metastasis. This paper unveils a novel inhibitor that effectively targets both RET and YES1, thereby demonstrating its potential to impede the growth and metastasis of RET rearrangement lung cancer.
    Journal
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    EGFR (Epidermal growth factor receptor) • KRAS (KRAS proto-oncogene GTPase) • ALK (Anaplastic lymphoma kinase) • RET (Ret Proto-Oncogene) • CCDC6 (Coiled-Coil Domain Containing 6) • CTTN (Cortactin)
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    EGFR mutation • ALK mutation • RET mutation • MET mutation • RET rearrangement • RET expression • RET positive
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    Tagrisso (osimertinib) • dasatinib • PLD-101
    over1year
    PLM-101 is a novel and potent FLT3/RET inhibitor with less adverse effects in the treatment of acute myeloid leukemia. (PubMed, Biomed Pharmacother)
    However, current FLT3-targeting agents, Midostaurin and Gilteritinib, face two significant issues, specifically the emergence of acquired resistance and drug-related adverse events leading to treatment failure...This study is the first to present a new FLT3/RET dual-targeting inhibitor, PLM-101, that shows potent anti-leukemic activity and fewer adverse effects. PLM-101, therefore, should be considered for use as a potential therapeutic agent for AML.
    Journal • Adverse events
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    FLT3 (Fms-related tyrosine kinase 3) • RET (Ret Proto-Oncogene)
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    FLT3 mutation
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    Xospata (gilteritinib) • Rydapt (midostaurin) • PLD-101