Target intelligence / Profile preview

Aurora kinase A (AURKA) (AURKA)

Target
AURKA
Molecular classification
Enzyme, Serine/threonine-protein kinase
01

Overview

Aurora kinase A (AURKA) is a critical serine/threonine kinase that regulates key stages of the cell cycle, particularly during mitosis. It is primarily localized to the centrosomes and spindle poles, where it facilitates centrosome maturation, spindle assembly, and the transition from G2 to M phase. AURKA is frequently overexpressed or amplified in a wide range of human malignancies, including breast, colon, and lung cancers, where it promotes genomic instability and aneuploidy. Beyond its role in cell division, AURKA is involved in non-mitotic pathways such as epithelial-mesenchymal transition (EMT) and the maintenance of cancer stem cell properties. Therapeutic strategies targeting AURKA involve small-molecule inhibitors like alisertib, which compete for the ATP-binding site to induce mitotic arrest and apoptosis. However, the clinical utility of these inhibitors is often limited by toxicities such as neutropenia and the challenge of identifying patients most likely to respond through specific biomarkers.

Other names
Serine/threonine-protein kinase 6STK6STK15Aurora 2AIKARK1AURABTAKPPP1R47STK7
02

Mechanism of action

ATP-competitive inhibition of the kinase domain, inhibition of autophosphorylation at Thr288, and disruption of the AURKA-TPX2 interaction.

03

Biological functions

Cell cycleCell proliferationOther
04

Disease associations

Cancer
05

Safety considerations

NeutropeniaSomnolenceMucositisBone marrow suppressionAlopeciaDiarrhea
06

Interacting drugs

Alisertib

6 more in the full profile.

07

Biomarkers

AURKA overexpressionPhospho-AURKA (Thr288)TPX2 expressionMYCN amplification

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