Aurora Kinases

Aurora kinases are a family of three highly homologous serine/threonine kinases that play a critical role in regulating many of the processes that are pivotal to mitosis. Each of the isoforms, Aurora A, Aurora B and Aurora C, has a different function in the control of mitosis.

Products
Background
Literature
Gene Data

Inhibitors

Cat No Product Name / Activity
4291 CCT 137690
Potent pan-Aurora kinase inhibitor
3988 Hesperadin hydrochloride
Potent Aurora kinase B inhibitor
3395 Lestaurtinib
Potent Aurora kinase A and B inhibitor; also inhibits JAK2, FLT3 and TrkA
4821 PF 03814735
Aurora kinase A and B inhibitor
4584 SNS 314 mesylate
Potent pan-Aurora kinase inhibitor
4066 TC-A 2317 hydrochloride
Potent, selective Aurora kinase A inhibitor
5286 TC-S 7010
Potent and selective Aurora kinase A inhibitor
5907 VX 680
High affinity and selective Aurora kinase inhibitor
2458 ZM 447439
Inhibits Aurora kinase B

Activators

Cat No Product Name / Activity
3084 Anacardic acid
Aurora kinase A activator. Also inhibits histone acetyltransferase

Aurora kinases are a family of three highly homologous serine/threonine kinases that play a critical role in regulating many of the processes that are pivotal to mitosis. Each isoform, Aurora A, Aurora B and Aurora C, has a different function in the control of this process.

Aurora A is involved in regulating many of the early mitotic events where its levels peak, particularly during the G2 phase. One target of Aurora A is cdc25b, a direct regulator of the cyclin B1-Cdk1 complex, which provides the basis for the role this enzyme plays in regulating entry into mitosis. Aurora A regulates centrosome maturation by moderating the recruitment of proteins, such as TPX-2, Ajuba, Bora and Lats, which are essential for accumulating microtubule spindle components, such as γ-tubulin. Aurora A is also associated with separation of centrosomes, through phosphorylation of the kinesin motor protein, Eg5. In addition, this enzyme regulates the microtubule network that forms mitotic spindles, through regulation of the EXTAH multiprotein complex.

Aurora B is the catalytic component of the chromosomal passenger complex (CPC) that is critical for the correct progression through and completion of mitosis. CPC is composed of three other proteins, survivin, INCENP and borealin, which are all substrates for Aurora B and function to regulate the activity of this enzyme. The CPC initially forms along chromosome arms, then concentrates at the centromere before finally localizing to the spindle midzone during cytokinesis. Functions of the CPC include condensation of chromosomes, formation of the bipolar spindle, attachment of the chromosomes to the mitotic spindle, regulation of the spindle checkpoint and completion of cytokinesis. An important target of Aurora B is histone H3, which is a critical regulator of chromosome condensation. H3 phosphorylation is a biomarker of Aurora B activity.

Aurora C is the least well studied member of this family and is expressed in most somatic tissues at levels much lower than Aurora A or B. However, expression is high in the testis, where this enzyme is thought to have a role in spermatozoa formation. During the cell cycle, the localization of Aurora C is dynamic and consistent with it being a CPC protein. In addition, Aurora C colocalizes with Aurora B during mitosis, suggesting that these isoforms may have an overlapping role with a degree of redundancy.

Since their discovery in the 1990s, Aurora kinases have been strongly linked to the progression of human cancers. Aurora A maps to human chromosome 20q13 and Aurora B to human chromosome 17q13.1, which are loci altered frequently in human cancers. Overexpression of Aurora A and B is seen in many cancers, but these enzymes are not oncoproteins, as concomitant oncogenic mutations are required to promote tumor progression. Aurora kinase inhibitors are an intense area of research for the development of cancer therapies.

Literature for Aurora Kinases

Cancer

Cancer Research Product Guide

A collection of over 750 products for cancer research, the guide includes research tools for the study of:

  • Cancer Metabolism
  • Epigenetics in Cancer
  • Receptor Signaling
  • Cell Cycle and DNA Damage Repair
  • Angiogenesis
  • Invasion and Metastasis
Kinases

Kinases Product Listing

A collection of over 400 products for kinase research, the listing includes inhibitors of:

  • Receptor Tyrosine Kinases
  • Protein Kinases A, C, D and G
  • PI-3 Kinase, Akt and mTOR
  • MAPK Signaling
  • Receptor Serine/Threonine Kinases
Cell Cycle & DNA Damage Repair

Cell Cycle & DNA Damage Repair Poster

In normal cells, each stage of the cell cycle is tightly regulated, however in cancer cells many genes and proteins that are involved in the regulation of the cell cycle are mutated or over expressed. Adapted from the 2015 Cancer Product Guide, Edition 3, this poster summarizes the stages of the cell cycle and DNA repair. It also highlights strategies for enhancing replicative stress in cancer cells to force mitotic catastrophe and cell death.

Aurora Kinase Gene Data

Gene Species Gene Symbol Gene Accession No. Protein Accession No.
Aurora Kinase A Human AURKA NM_003600 O14965
Mouse Aurka NM_011497 P97477
Rat Aurka NM_153296 P59241
Aurora Kinase B Human AURKB NM_004217 Q96GD4
Mouse Aurkb NM_011496 O70126
Rat Aurkb NM_053749 O55099
Aurora Kinase C Human AURKC NM_003160 Q9UQB9
Mouse Aurkc NM_001080966 O88445
Rat Aurkc NM_001106221 -