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    DRUG:

    CHR-6494

    i
    Other names: CHR-6494
    Company:
    Kansai Medical University
    Drug class:
    Haspin inhibitor
    almost2years
    Novel inhibitors targeting the PGK1 metabolic enzyme in glycolysis exhibit effective antitumor activity against kidney renal clear cell carcinoma in vitro and in vivo. (PubMed, Eur J Med Chem)
    Our previous research has revealed phosphoglycerate kinase 1 (PGK1) enhances tumorigenesis and sorafenib resistance of kidney renal clear cell carcinoma (KIRC) by regulating glycolysis, so that PGK1 is a promising drug target. Z57346765 induced expression changes of genes related to cell metabolism, DNA replication and cell cycle. Overall, we screened two novel PGK1 inhibitors, CHR-6494 and Z57346765, for the first time and discovered their potent anti-KIRC effects by suppressing PGK1 metabolic enzyme activity in glycolysis.
    Preclinical • Journal
    |
    PGK1 (Phosphoglycerate Kinase 1)
    |
    sorafenib • CHR-6494
    3years
    Co-inhibition of Aurora A and Haspin kinases enhances survivin blockage and p53 induction for mitotic catastrophe and apoptosis in human colorectal cancer. (PubMed, Biochem Pharmacol)
    Co-treatment of CHR6494 and MLN8237 enhanced the blockage of human CRC xenograft tumors in nude mice. Taken together, co-inhibition of Aurora A and Haspin enhances survivin inhibition, p53 pathway induction, mitotic catastrophe, apoptosis and tumor inhibition that may provide a potential strategy for CRC therapy.
    Journal
    |
    BIRC5 (Baculoviral IAP repeat containing 5) • HASPIN (Histone H3 Associated Protein Kinase)
    |
    BIRC5 expression • HASPIN expression
    |
    alisertib (MLN8237) • CHR-6494