Molecular Target Synopsis
Overview
Domains and Structures
Drugs and Clinical Candidates
Druggability
Chemistry
Ligand Efficiency Plot
Pathways
Family Cladogram
Interaction Network
Gene Expression
Gene Copy Number Variation
RNAi
Mutations
Germline Genetics

Aurka (P97477) - Overview - Molecular Target Synopsis

Protein


Aurka, Aurora kinase A
Enzyme Classification 2.7.11.1
UniProt P97477

Also Known as AURKA_MOUSE, Aurka, Aik, Airk, Ark1, Aura, Ayk1, Btak, Iak1, Stk15, Stk6

Mitotic serine/threonine kinase that contributes to the regulation of cell cycle progression. Associates with the centrosome and the spindle microtubules during mitosis and plays a critical role in various mitotic events including the establishment of mitotic spindle, centrosome duplication, centrosome separation as well as maturation, chromosomal alignment, spindle assembly checkpoint, and cytokinesis. Required for normal spindle positioning during mitosis and for the localization of NUMA1 and DCTN1 to the cell cortex during metaphase (By similarity). Required for initial activation of CDK1 at centrosomes. Phosphorylates numerous target proteins, including ARHGEF2, BORA, BRCA1, CDC25B, DLGP5, HDAC6, KIF2A, LATS2, NDEL1, PARD3, PPP1R2, PLK1, RASSF1, TACC3, p53/TP53 and TPX2. Regulates KIF2A tubulin depolymerase activity. Required for normal axon formation. Plays a role in microtubule remodeling during neurite extension. Important for microtubule formation and/or stabilization. Also acts as a key regulatory component of the p53/TP53 pathway, and particularly the checkpoint-response pathways critical for oncogenic transformation of cells, by phosphorylating and stabilizing p53/TP53. Phosphorylates its own inhibitors, the protein phosphatase type 1 (PP1) isoforms, to inhibit their activity. Necessary for proper cilia disassembly prior to mitosis. Interacts with CPEB1, JTB, TACC1, TPX2, PPP2CA, as well as with the protein phosphatase type 1 (PP1) isoforms PPP1CA, PPP1CB and PPP1CC (By similarity). Interacts also with its substrates ARHGEF2, BORA, BRCA1, KIF2A, PARD3, and p53/TP53. Interaction with BORA promotes phosphorylation of PLK1. Interacts with GADD45A, competing with its oligomerization (By similarity). Interacts with FBXL7 and PIFO. Interacts (via C-terminus) with AUNIP (via C-terminus) (By similarity). Identified in a complex with AUNIP and NIN (By similarity). Interacts with SIRT2 (By similarity). Interacts with FRY; this interaction facilitates AURKA-mediated PLK1 phosphorylation. Interacts with MYCN; interaction is phospho-independent and triggers AURKA activation; AURKA competes with FBXW7 for binding to unphosphorylated MYCN but not for binding to phosphorylated MYCN (By similarity). Interacts with HNRNPU.

3D2K
CRYSTAL STRUCTURE OF MOUSE AURORA A (ASN186->GLY, LYS240- >ARG, MET302->LEU) IN COMPLEX WITH [7-(2-{2-[3-(3-CHLORO- PHENYL)-UREIDO]-THIAZOL-5-YL}-ETHYLAMINO)-PYRAZOLO[4,3- D]PYRIMIDIN-1-YL]-ACETIC ACID
RCSB/PDB
Inspect Structure
See all 3D Structures for Aurka

Isoforms / Transcripts (Protein Coding)


Protein Length Ensembl Gene Ensembl Transcript Ensembl Protein Uniprot Isoform
417P97477-2
395P97477-1

Sub-cellular localization


UniProt: Aurka is active in the following subcellular-locations: centriole, centrosome, cilium basal body, cytoplasm, cytoskeleton, microtubule organizing center, spindle pole.
GO terms: Aurka is active in the following subcellular-locations: axon hillock, centriole, centrosome, chromosome passenger complex, cilium, condensed nuclear chromosome, cytosol, germinal vesicle, meiotic spindle, microtubule cytoskeleton, microtubule organizing center, mitotic spindle, mitotic spindle pole, nucleoplasm, nucleus, perinuclear region of cytoplasm, pronucleus, spindle, spindle microtubule, spindle midzone, spindle pole centrosome.



UniProt
GO terms

Gene Copy Number Variation


In COSMIC - Cell Lines Project Aurka has gain in 0 cell-lines, loss in 0 cell-lines and no signal in 0 cell-lines. (see details)

3D Structures


For Aurka there are:
8 structures (8 chains) solved
8 are solved in complex with at least one small molecule ligand



(see details)
Molecular Target 3D Synopsis

Screening and Chemistry


Aurka has been screened with 54 compounds (59 bioactivities), 42 compounds have bioactivities that show binding affinity of <= 500nM (47 bioactivities). (see details)