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Journal: Design, synthesis and biological evaluation of MNK-PROTACs. (Pubmed Central) - Dec 20, 2024 In this study, DS33059, a small-molecule compound modified based on the ongoing clinical trials drug ETC-206, was chosen as the target protein ligand...The protein degradation assay showed that compound II-5 had good capability to degrade MNK1. The MNK-PROTACs strategy represents a new direction in treating tumors and deserves further exploration.
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Reclaiming a dirty drug: What is the context of vulnerability to arsenic trioxide in glioblastoma? (Section 29) - Mar 5, 2024 - Abstract #AACR2024AACR_6827; These findings further implicate MNK1 activity and cellular response to oxidative stress as markers of ATO sensitivity, however they are not the sole determinates of response. Understanding of the mechanism of action for idiopathic compounds may allow for the discovery of molecular signatures of sensitivity, improving patient selection for clinical trials and the development of new combination approaches to combat resistance in other tumor types.
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AUM001 potentiates the anti-tumor activity of gemcitabine in an AsPC-1 PDAC model (Poster HALL LEVEL 0) - May 6, 2023 - Abstract #ESMOGI2023ESMO_GI_580; Pharmacodynamic analysis suggests that AUM001 may potentiate the reduction in pro-tumorigenic protein expression and slow the tumor growth kinetics. This is the first study depicting clinical activity of AUM001 in combination with chemotherapy for the treatment of PDAC.
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