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

National Center For Advancing Translational Sciences

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Abstract

The NCATS Early Translation Branch (ETB) hosts a broad and comprehensive program for the discovery of drug candidates directed towards rare diseases and pharmacological tools to probe the function of the human genome. ETB conducts research to understand the underlying principles driving the translation of basic research discoveries into tangible improvements in human health. During the reporting period, the collaborative team has developed novel allosteric inhibitors of cAbl capable of crossing the blood-brain barrier. A number of these were found to have good CNS penetration and pharmacokinetic properties. Further high-throughput screening was performed using brain tumor initiating cells, and combination studies with cAbl modulators were conducted to further explore this therapeutic modality.