Cyclin dependent kinase 4 (complex with cyclin D1)
Synonyms: cell division protein kinase 4
CDK4 is a serine/threonine protein kinase and a member of cyclin dependent kinase family. Active complex of CDK4 with cyclin D1 is required to maintain breast tumorigenesis1. CDK4 is closely related to CDK6 – both are cyclin D dependent kinases and are both active in the first gap phase (G1) 2. CDK4 has surprisingly narrow activity – it phosphorylates mainly the retinoblastoma protein (RB1, hereafter RB) and two other RB-family proteins. The first selective inhibitor for CDK4 and CDK6 is Abemaciclib, which the safety and antitumor activity of abemaciclib as a single agent was demonstrated3.
CDK4-CYCLIND1 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. Yu Q, Sicinska E, Geng Y, Ahnström M, Zagozdzon A, Kong Y, Gardner H, Kiyokawa H, Harris LN, Stål O, Sicinski P. Requirement for CDK4 kinase function in breast cancer. Cancer cell. 2006 Jan 31;9(1):23-32.
2. Sherr CJ, Beach D, Shapiro GI. Targeting CDK4 and CDK6: from discovery to therapy. Cancer discovery. 2016 Apr 1;6(4):353-67.
3. 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.