Aurora kinase inhibitors.
Most human cancer cells are characterized by changes in the amount or organization of DNA resulting in chromosome instability and aneuploidy. Several mitotic kinases, Aurora kinases amongst others, regulate the progression of the cell through mitosis. So far three Aurora kinases have been identified in man: Aurora-A, Aurora-B and Aurora-C. Aurora kinases were recently identified as a potential target in anticancer therapy, and various Aurora-A and Aurora-B kinase inhibitors are in development. In this review we provide a brief insight into the mechanism of action as far as currently available. We review the available pre-clinical data, discuss the clinical phase I data and try to give a direction for future headings.
Department of Medical Oncology, Erasmus University Medical Center, EA Rotterdam, The Netherlands.
J J E M
JJ
Kitzen
M J A
MJ
de Jonge
J
J
Verweij
D000818:Animals; D064107:Aurora Kinase B; D064108:Aurora Kinase C; D064127:Aurora Kinases; D017321:Clinical Trials, Phase I as Topic; D004353:Drug Evaluation, Preclinical; D006801:Humans; D008297:Male; D008954:Models, Biological; D009369:Neoplasms / Q000188:drug therapy* / Q000378:metabolism; D047428:Protein Kinase Inhibitors / Q000494:pharmacology / Q000627:therapeutic use*; D017346:Protein Serine-Threonine Kinases / Q000037:antagonists & inhibitors* / Q000378:metabolism / Q000502:physiology
D047428:Protein Kinase Inhibitors; C576921:AURKB protein, human; C576927:AURKC protein, human; D064107:Aurora Kinase B; D064108:Aurora Kinase C; D064127:Aurora Kinases; D017346:Protein Serine-Threonine Kinases