^
    almost4years
    [VIRTUAL] Discovery of GT19077, a c-Myc/Max protein-protein Interaction (PPI) small molecule inhibitor, and GT19506 a c-Myc PROTAC molecule, for targeting c-Myc-driven blood cancers and small cell lung cancers (AACR 2021)
    In conclusion, GT19077 and GT19506 are currently in Lead Optimization Phase, which demonstrate the desired selectivity of targeting Myc dependent B-cell malignancies and Myc-amplified SCLC, but sparing c-Myc in growth factor/cytokine regulated blood progenitor cells. The defined selectivity has enabled the ongoing in vivo efficacy studies, currently GT19077 and GT19506 have being evaluated in in vivo efficacy studies.
    PD(L)-1 Biomarker • IO biomarker
    |
    MYC (V-myc avian myelocytomatosis viral oncogene homolog) • MYCN (MYCN Proto-Oncogene BHLH Transcription Factor) • CD47 (CD47 Molecule) • MYCL (MYCL Proto-Oncogene BHLH Transcription Factor)
    |
    GT19077
    4years
    [VIRTUAL] Discovery of GT19077, a c-Myc/Max Protein-Protein Interaction (PPI) Small Molecule Inhibitor, for Targeting c-Myc-Driven Blood Cancers (ASH 2020)
    GT19077 was also much less active at degrading c-Myc in GM-CSF-stimulated TF-1 or IL-2-stimulated lymphoid progenitor NK-92 cells assayed by WB. These results can help develop biomarkers for patient tailoring strategy. Finally, GT19077 demonstrates PK-dependent target engagement in vivo and is currently being evaluated in in vivo efficacy studies.
    PD(L)-1 Biomarker • IO biomarker
    |
    KRAS (KRAS proto-oncogene GTPase) • MYC (V-myc avian myelocytomatosis viral oncogene homolog) • FGFR (Fibroblast Growth Factor Receptor) • IL2 (Interleukin 2)
    |
    KRAS mutation • FGFR fusion • KRAS G12A • KRAS G12 • MYC expression • JAK2 V617F
    |
    GT19077 • Neukoplast (CST-101)