title: Aurora kinase inhibitors as anti-cancer therapy.
abstract: Aurora kinases are serine and threonine kinases that function as key regulators of the mitosis process. There are three distinct human aurora kinases known as Aurora A, Aurora B, and Aurora C. Aurora A and Aurora B are overexpressed in a number of human cancers including non-small cell lung cancer, glioblastomas, and upper gastrointestinal adenocarcinomas. Given their association with tumorigenesis, both Aurora A and Aurora B have been targeted for cancer therapy. Currently, a number of selective and nonselective aurora kinase inhibitors are being tested in preclinical and clinical settings as anti-tumor agents. We review the biology of human aurora kinases, followed by an overview of inhibitors undergoing current clinical investigations.
authors.affiliation: Departments of Medical Oncology, Yale University School of Medicine, 333 Cedar Street, New Haven, CT 06520, USA.
authors.forename: Warren
authors.initials: W
authors.lastname: Lok
authors.forename: Rhonda Q
authors.initials: RQ
authors.lastname: Klein
authors.forename: Muhammad Wasif
authors.initials: MW
authors.lastname: Saif
mesh_terms: D000970:Antineoplastic Agents / Q000494:pharmacology / Q000627:therapeutic use*; D064107:Aurora Kinase B; D064108:Aurora Kinase C; D064127:Aurora Kinases; D001549:Benzamides / Q000494:pharmacology / Q000627:therapeutic use; D001562:Benzimidazoles / Q000494:pharmacology / Q000627:therapeutic use; D003509:Cyclohexanecarboxylic Acids / Q000494:pharmacology / Q000627:therapeutic use; D004354:Drug Screening Assays, Antitumor; D004789:Enzyme Activation; D006801:Humans; D009369:Neoplasms / Q000188:drug therapy* / Q000201:enzymology; D010755:Organophosphates / Q000494:pharmacology / Q000627:therapeutic use; D010671:Phenylurea Compounds / Q000494:pharmacology / Q000627:therapeutic use; D047428:Protein Kinase Inhibitors / Q000494:pharmacology / Q000627:therapeutic use*; D017346:Protein Serine-Threonine Kinases / Q000037:antagonists & inhibitors* / Q000378:metabolism; D011720:Pyrazoles / Q000494:pharmacology / Q000627:therapeutic use; D011799:Quinazolines / Q000494:pharmacology / Q000627:therapeutic use; D013844:Thiazoles / Q000494:pharmacology / Q000627:therapeutic use; D014508:Urea / Q000031:analogs & derivatives / Q000494:pharmacology / Q000627:therapeutic use
chemical_list: C535237:1-cyclopropyl-3-(3-(5-morpholin-4-ylmethyl-1H-benzoimidazol-2-yl)-1H-pyrazol-4-yl)urea; C520647:2-((3-((4-((5-(2-((3-fluorophenyl)amino)-2-oxoethyl)-1H-pyrazol-3-yl)amino)quinazolin-7-yl)oxy)propyl)(ethyl)amino)ethyl dihydrogen phosphate; C547876:4-(3-chloro-2-fluorophenoxy)-1-((6-(1,3-thiazol-2-ylamino)pyridin to 2-yl)methyl) cyclohexanecarboxylic acid; D000970:Antineoplastic Agents; D001549:Benzamides; D001562:Benzimidazoles; D003509:Cyclohexanecarboxylic Acids; D010755:Organophosphates; D010671:Phenylurea Compounds; D047428:Protein Kinase Inhibitors; D011720:Pyrazoles; D011799:Quinazolines; C532454:SNS 314; D013844:Thiazoles; D014508:Urea; C576921:AURKB protein, human; C576927:AURKC protein, human; D064107:Aurora Kinase B; D064108:Aurora Kinase C; D064127:Aurora Kinases; D017346:Protein Serine-Threonine Kinases; C523797:danusertib