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

HASPIN (Q8TF76) - Overview - Molecular Target Synopsis

Protein


HASPIN, Serine/threonine-protein kinase haspin
Enzyme Classification 2.7.11.1
UniProt Q8TF76

Also Known as HASP_HUMAN, HASPIN, GSG2

Serine/threonine-protein kinase that phosphorylates histone H3 at 'Thr-3' (H3T3ph) during mitosis. May act through H3T3ph to both position and modulate activation of AURKB and other components of the chromosomal passenger complex (CPC) at centromeres to ensure proper chromatid cohesion, metaphase alignment and normal progression through the cell cycle.

6G39
CRYSTAL STRUCTURE OF HASPIN F605Y MUTANT IN COMPLEX WITH 5- IODOTUBERCIDIN
RCSB/PDB
Inspect Structure
See all 3D Structures for HASPIN

Isoforms / Transcripts (Protein Coding)


Protein Length Ensembl Gene Ensembl Transcript Ensembl Protein Uniprot Isoform
810ENSG00000177602ENST00000325418ENSP00000325290
798Q8TF76-1
314Q8TF76-2

Sub-cellular localization


UniProt: HASPIN is active in the following subcellular-locations: chromosome, cytoplasm, cytoskeleton, nucleus, spindle.
GO terms: HASPIN is active in the following subcellular-locations: centrosome, chromosome, cytoplasm, nucleus, spindle.



UniProt
GO terms

Gene Copy Number Variation


In COSMIC - Cell Lines Project HASPIN has gain in 0 cell-lines, loss in 3 cell-lines and no signal in 1002 cell-lines. (see details)

Gene Expression


In NCI60, the highest expressing cell lines are:

In Array Express (RNA-seq of 675 commonly used human cancer cell lines), the highest expressing cell lines are:

In Array Express (RNA-seq of long poly adenylated RNA and long non poly adenylated RNA from ENCODE cell lines), the highest expressing cell lines are:

(see details)

RNA Interference


HASPIN was reported in the following RNAI studies:

Cell - Large Scale Profiling of Kinase Dependencies in Cancer Cell Lines, the highest RNAi cell lines are: VP229, RMGI. (see details)

3D Structures


For HASPIN there are:
18 structures (18 chains) solved
15 are solved in complex with at least one small molecule ligand
1 are solved with an approved drug

HASPIN is solved in complex with the approved drug(s):

AMP/ADENOSINE PHOSPHATE (3DLZ_A).

(see details)
Molecular Target 3D Synopsis

Screening and Chemistry


HASPIN has been screened with 263 compounds (425 bioactivities), 16 compounds have bioactivities that show binding affinity of <= 500nM (16 bioactivities). (see details)