Cyclin dependent kinase 6 (complex with cyclin D3)
Synonyms: cell division protein kinase 6, PLSTIRE
CDK6 is a serine/threonine protein kinase and a member of cyclin dependent kinase family. CDK6 is closely related to CDK4 – both are cyclin D dependent kinases and are both active in the first gap phase (G1)1. It was proposed that CDK4/6-cyclin D complex phosphorylates the retinoblastoma tumour suppressor, causing it to dissociate from E2F transcription factors, affecting DNA replication and cell division2. The first selective inhibitor for CDK4 and CDK6 is Abemaciclib, which the safety and antitumor activity of abemaciclib as a single agent was demonstrated3.
CDK6-CYCLIND3 kinase assay is run on mobility shift microfluidics platform (Caliper), which provides best in industry quality of data. We routinely run services associated with this kinase including: screening, profiling, dose-response studies and kinetic measurements. Please contact us for more information.
1. Sherr CJ, Beach D, Shapiro GI. Targeting CDK4 and CDK6: from discovery to therapy. Cancer discovery. 2016 Apr 1;6(4):353-67.
2. Yin L, Li H, Liu W, Yao Z, Cheng Z, Zhang H, Zou H. A highly potent CDK4/6 inhibitor was rationally designed to overcome blood brain barrier in gliobastoma therapy. European journal of medicinal chemistry. 2017 Dec 6.
2. Patnaik A, Rosen LS, Tolaney SM, Tolcher AW, Goldman JW, Gandhi L, Papadopoulos KP, Beeram M, Rasco DW, Hilton JF, Nasir A. Efficacy and safety of abemaciclib, an inhibitor of CDK4 and CDK6, for patients with breast cancer, non–small cell lung cancer, and other solid tumors. Cancer discovery. 2016 Jul 1;6(7):740-53.