The efficacy of the cyclin-dependent kinase 4/6 inhibitor in endometrial cancer

• DOI: 10.1371/journal.pone.0177019
• Publication Date: 2017-05-04T18:16:17Z
• Authors: Tomohito Tanaka; Yoshito Terai; Keisuke Ashihara; Satoe Fujiwara; Yoshimichi Tanaka; Hiroshi Sasaki; Satoshi Tsunetoh; Masahide Ohmichi
• Keywords: Palbociclib; Retinoblastoma protein; Retinoblastoma; Cyclin-dependent kinase 4

Background PD-0332991, the selective cyclin-dependent kinase 4/6 inhibitor palbociclib, causes cell cycle arrest by inhibiting phosphorylation of retinoblastoma (Rb) protein. The aim this study was to evaluate therapeutic potential PD-0332991 in endometrial cancer. Methods and findings Four human cancer lines, ECC, HEC1A, HEC108 TEN, were treated with their function evaluated. In vivo, efficacy evaluated a model subcutaneous An immunohistochemical analysis performed 337 specimens. A proliferation assay revealed that 2 4 lines expressed Rb sensitive an IC50 0.65 μM (HEC1A) 0.58 (HEC108), respectively. Both had G0/G1 after treatment according flow cytometry. antitumoral reduction activity Ki67 Rb. Immunohistochemical analyses positive rate 67.7%, however, there no significant relationship between expression levels tumor grade. Conclusions against expressing Our approximately 70% patients might have indications for PD-0332991. Of note, grade impact on treatment.