Characterizing inhibitors of tyrosine protein kinase ABL1 (ABL1) in human glioblastoma

National Center For Advancing Translational Sciences

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Abstract

NCATS has developed novel allosteric inhibitors of cAbl that are able to cross the blood-brain barrier. A number of these allosteric inhibitors of wild type cAbl kinase that NCATS developed were found to have good CNS penetration and good pharmacokinetic properties. These compounds were sent to Dr. Klonish for evaluation of biological activity in context of glioblastoma. During the this period, NCATS developed a high-throughput assay to examine glioblastoma cytotoxicity for brain tumor initiating cells. Analogs were also tested in U251 glioblastoma cells.