RON inhib News - LARVOL Sigma

|||||||||| Xalkori (crizotinib) / Pfizer
Differential Requirements for the RON Ligand Binding and Kinase Domains in Myeloproliferative Neoplasms (Halls G-H (San Diego Convention Center)) - Nov 6, 2024 - Abstract #ASH2024ASH_5874;
Consistent with these results, pharmacological inhibition of RON with the MET/RON inhibitor crizotinib significantly decreased disease burden in MPLW515L mice...This work highlights an important role for RON activity in MPN disease progression, which appears to be specifically related to ligand-independent signaling in the setting of PMF driven by MPLW515L. The promising survival benefits and minimal hematopoietic toxicity associated with genetic inactivation of RON kinase activity in vivo support further investigation of RON inhibitors in PMF.

|||||||||| Journal: Oroxylin A suppresses breast cancer-induced osteoclastogenesis and osteolysis as a natural RON inhibitor. (Pubmed Central) - May 29, 2024
Our results indicate that OA acts as a natural RON inhibitor to suppress breast cancer-induced osteoclastogenesis and osteolysis. This provides new strategy for treating breast cancer-induced bone destruction and related syndromes.

|||||||||| Development of a novel, selective, and potent inhibitor of RON kinase (Section 25) - Mar 5, 2024 - Abstract #AACR2024AACR_2727;
This provides new strategy for treating breast cancer-induced bone destruction and related syndromes. ZB-60 has target specific activity and exhibits favorable drug-like properties.

|||||||||| ASLAN002 / BMS
Journal, Metastases: RON-augmented cholesterol biosynthesis in breast cancer metastatic progression and recurrence. (Pubmed Central) - Apr 8, 2023
BMS777607, a RON inhibitor, abrogated CTC colony formation tumor cells and tumor recurrence...In mouse models with RON overexpression, statin-mediated inhibition of cholesterol biosynthesis impeded metastatic progression and recurrence but does not affect the primary tumor. RON upregulates glycolysis and cholesterol biosynthesis gene expression by two pathways: MAPK-dependent c-Myc expression and ?-catenin -dependent SREBP2 expression.

|||||||||| RON receptor tyrosine kinase in head and neck cancer: a potential target for overcoming resistance to anti-EGFR therapy (Section 14; Poster Board #3) - Mar 14, 2023 - Abstract #AACR2023AACR_2480;
Protein expression data and in silica analyses support an inverse association between EGFR and RON. RON expression is associated with radiation resistance.



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