ArQule announces publication of ARQ531 preclinical data.
ArQule announced the publication of preclinical study data for ARQ 531, the Company's rationally-designed, reversible inhibitor of both wild type and C481S-mutant Bruton's tyrosine kinase. The studies, published in Cancer Discovery, were conducted in collaboration with researchers at The Ohio State University. Data from these studies demonstrated efficacy in in vitro and in vivo hematologic malignancy models that recapitulate the most common mechanisms of resistance to irreversible BTK inhibitors, including ibrutinib. Highlights from the manuscript (link here) include: 1)The crystal structure of ARQ 531 bound to BTK elucidates the mechanism of BTK inhibition that is not dependent on the specific amino acid residue at position 481. 2) Recombinant BTK biochemical assays of ARQ 531 and ibrutinib show similar inhibition for wild type BTK, however ibrutinib has dramatically lower inhibition, binding affinity and residence time for mutant BTK.
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|Date:||Aug 13, 2018|
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