Search Results - "Ballard, Joshua A"
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Inhibition and Binding Kinetics of the Hepatitis C Virus NS3 Protease Inhibitor ITMN-191 Reveals Tight Binding and Slow Dissociative Behavior
Published in Biochemistry (Easton) (24-03-2009)“…The protease activity of hepatitis C virus nonstructural protein 3 (NS3) is essential for viral replication. ITMN-191, a macrocyclic inhibitor of the NS3…”
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Preclinical characterization of pirtobrutinib, a highly selective, noncovalent (reversible) BTK inhibitor
Published in Blood (06-07-2023)“…•Pirtobrutinib is a potent, noncovalent (reversible), highly selective inhibitor of BTK and C481-mutant BTK.•Pirtobrutinib is efficacious in B-cell models…”
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Pirtobrutinib preclinical characterization: a highly selective, non-covalent (reversible) BTK inhibitor
Published in Blood (16-02-2023)“…Bruton tyrosine kinase (BTK), a nonreceptor tyrosine kinase, is a major therapeutic target for B-cell driven malignancies. However, approved covalent BTK…”
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Abstract 1464: Pre-clinical characterization of potent and selective next-generation RET inhibitors
Published in Cancer research (Chicago, Ill.) (01-07-2021)“…Abstract In May 2020, selpercatinib became the first FDA-approved selective RET inhibitor, indicated for patients (pts) with RET fusion-positive NSCLC and…”
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Abstract P141: Preclinical characterization of LOX-24350, a highly potent and isoform-selective FGFR3 inhibitor
Published in Molecular cancer therapeutics (01-12-2021)“…Abstract Alterations in the fibroblast growth factor receptors (FGFRs) have been identified as oncogenic drivers in many human cancers. Specifically,…”
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Abstract 2780: Unique pharmacodynamic properties conferred by differential binding to BTK, pirtobrutinib vs covalent inhibitors
Published in Cancer research (Chicago, Ill.) (04-04-2023)“…Abstract Covalent Bruton tyrosine kinase inhibitors (cBTKi) have transformed the treatment of B cell malignancies. Despite the efficacy of cBTKi, treatment…”
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The KRAS G12C Inhibitor MRTX849 Provides Insight toward Therapeutic Susceptibility of KRAS-Mutant Cancers in Mouse Models and Patients
Published in Cancer discovery (01-01-2020)“…Despite decades of research, efforts to directly target KRAS have been challenging. MRTX849 was identified as a potent, selective, and covalent KRAS inhibitor…”
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