Biperiden ROTAC for CDK6 Epub 2014 Oct 5

Epub 2014 Oct 5

T16A(inh)-A01

Significant inhibition of proliferation of the AR-positive prostate cancer cell lines LNCaP and VCaP with doses of Abiraterone ≥5 μM is confirmed

which leads to a conformational change in the EED H3K27me3-binding pocket and prevents the interaction of EED with the histone methyltransferase enhancer zeste homolog 2 (EZH2)

Biperiden ROTAC for CDK6 Epub 2014 Oct 5AZD8186 is and inhibitor of the beta isoform of phosphoinositide 3 kinase (PI3K), with potential antineoplastic activity. Upon administration, PI3Kbeta inhibitor AZD8186 selectively inhibits the activity of PI3Kbeta in the PI3K Akt mTOR signaling pathway, which may result in a decrease of tumor cell proliferation. It also induces cell death in PI3K expressing cancer cells. By specifically targeting class I PI3K beta, this agent may be more efficacious