論文掲載：テキサス大学MD Anderson Cancer Center、優れた薬物動態学的および物理化学的特性を有する臨床段階の選択的グルタミナーゼ-1（GLS-1）阻害剤「IPN60090」の創製

Journal of Medicinal Chemistry
October 29, 2020

Inhibition of glutaminase-1 (GLS-1) hampers the proliferation of tumor cells reliant on glutamine. Known glutaminase inhibitors have potential limitations, and in vivo exposures are potentially limited due to poor physicochemical properties. We initiated a GLS-1 inhibitor discovery program focused on optimizing physicochemical and pharmacokinetic properties, and have developed a new selective inhibitor, Compound 27 (IPN60090), which is currently in phase 1 clinical trials. Compound 27 attains high oral exposures in preclinical species, with strong in vivo target engagement, and should robustly inhibit glutaminase in humans.

In this work, Genedata Screener was used in multiple assays: dual-coupled enzyme assay, cell viability assay, and cellular target engagement assay.