Description
Palbociclib is an inhibitor of CDK4 and CDK6 that displays anticancer chemotherapeutic and nephroprotective activities; it is currently in clinical trials as a potential treatment for breast cancer. Palbociclib induces G0/G1 phase cell cycle arrest in renal proximal tubule cells, protecting animals against nephrotoxicity and inflammation induced by other chemotherapeutics. Palbociclib also induces cell cycle arrest in cellular and animal models of glioma, increasing overall survival times. In animal models of retinoblastoma, this compound inhibits cell proliferation, and induces G1 phase cell cycle arrest and tumor regression.
References
Vaughn DJ, Hwang W, Lal P, et al. Phase 2 trial of the cyclin-dependent kinase 4/6 inhibitor palbociclib in patients with retinoblastoma protein-expressing germ cell tumors. Cancer. 2014 Dec 18. [Epub ahead of print]. PMID: 25522918.
DiRocco DP, Bisi J, Roberts P, et al. CDK4/6 inhibition induces epithelial cell cycle arrest and ameliorates acute kidney injury. Am J Physiol Renal Physiol. 2014 Feb 15;306(4):F379-88. PMID: 24338822.
Barton KL, Misuraca K, Cordero F, et al. PD-0332991, a CDK4/6 inhibitor, significantly prolongs survival in a genetically engineered mouse model of brainstem glioma. PLoS One. 2013 Oct 2;8(10):e77639. PMID: 24098593.
Fry DW, Harvey PJ, Keller PR, et al. Specific inhibition of cyclin-dependent kinase 4/6 by PD 0332991 and associated antitumor activity in human tumor xenografts. Mol Cancer Ther. 2004 Nov;3(11):1427-38. PMID: 15542782.
