Cyclopenta[ b]indole Derivative Inhibits Aurora B in Primary Cells
Journal article, 2020

The Aurora family of kinases is closely involved in regulating cell division. Inhibition of Aurora A and B with small molecules is currently being investigated in clinical trials for the treatment of different cancers. It has also been evaluated as a treatment option against different autoimmune diseases in preclinical studies. Here, we present a cyclopenta[b]indole derivative capable of inhibiting Aurora B selectively in kinase assays. To evaluate the Aurora B inhibition capacity of the compound, we used a kinase IC50 assay as well as a suppression assay of proliferating primary cells. In addition, we examined if the cells had gained a phenotype characteristic for Aurora B inhibition after treatment with the compound. We found that the compound selectively inhibited Aurora B (IC50 = 1.4 μM) over Aurora A (IC50 > 30 μM). Moreover, the compound inhibited proliferating PBMCs with an IC50 = 4.2 μM, and the cells displayed reduced phosphorylation of histone H3 as well as tetraploidy, consistent with Aurora B inhibition.


Andreas Ekebergh

Chalmers, Chemistry and Chemical Engineering, Chemistry and Biochemistry

Jerker Mårtensson

Chalmers, Chemistry and Chemical Engineering, Chemistry and Biochemistry

Christine Lingblom Ekebergh

University of Gothenburg

Sahlgrenska University Hospital

ACS Omega

24701343 (eISSN)

Vol. 5 51 33455-33460

Subject Categories

Cell and Molecular Biology

Pharmacology and Toxicology

Medical Biotechnology (with a focus on Cell Biology (including Stem Cell Biology), Molecular Biology, Microbiology, Biochemistry or Biopharmacy)





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