Details of the Target

General Information of Target

Target ID LDTP11897
Target Name Homeodomain-interacting protein kinase 3 (HIPK3)
Gene Name HIPK3
Gene ID 10114
Synonyms
DYRK6; FIST3; PKY; Homeodomain-interacting protein kinase 3; EC 2.7.11.1; Androgen receptor-interacting nuclear protein kinase; ANPK; Fas-interacting serine/threonine-protein kinase; FIST; Homolog of protein kinase YAK1
3D Structure
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2D Sequence (FASTA)
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3D Structure (PDB)
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Sequence
MTSVTRSEIIDEKGPVMSKTHDHQLESSLSPVEVFAKTSASLEMNQGVSEERIHLGSSPK
KGGNCDLSHQERLQSKSLHLSPQEQSASYQDRRQSWRRASMKETNRRKSLHPIHQGITEL
SRSISVDLAESKRLGCLLLSSFQFSIQKLEPFLRDTKGFSLESFRAKASSLSEELKHFAD
GLETDGTLQKCFEDSNGKASDFSLEASVAEMKEYITKFSLERQTWDQLLLHYQQEAKEIL
SRGSTEAKITEVKVEPMTYLGSSQNEVLNTKPDYQKILQNQSKVFDCMELVMDELQGSVK
QLQAFMDESTQCFQKVSVQLGKRSMQQLDPSPARKLLKLQLQNPPAIHGSGSGSCQ
Target Bioclass
Enzyme
Family
Protein kinase superfamily, CMGC Ser/Thr protein kinase family, HIPK subfamily
Subcellular location
Cytoplasm
Function
Serine/threonine-protein kinase involved in transcription regulation, apoptosis and steroidogenic gene expression. Phosphorylates JUN and RUNX2. Seems to negatively regulate apoptosis by promoting FADD phosphorylation. Enhances androgen receptor-mediated transcription. May act as a transcriptional corepressor for NK homeodomain transcription factors. The phosphorylation of NR5A1 activates SF1 leading to increased steroidogenic gene expression upon cAMP signaling pathway stimulation. In osteoblasts, supports transcription activation: phosphorylates RUNX2 that synergizes with SPEN/MINT to enhance FGFR2-mediated activation of the osteocalcin FGF-responsive element (OCFRE).
Uniprot ID
Q9H422
Ensemble ID
ENST00000303296.9
HGNC ID
HGNC:4915
ChEMBL ID
CHEMBL4577

Target Site Mutations in Different Cell Lines

Cell line Mutation details Probe for labeling this protein in this cell
A549 SNV: p.D713G .
CHL1 SNV: p.P107L .
COLO800 SNV: p.S936G .
HCC1954 SNV: p.Q142R .
HUCCT1 SNV: p.G892D .
Ishikawa (Heraklio) 02 ER Insertion: p.C434LfsTer20 .
MEWO SNV: p.L488R .
MFE319 SNV: p.G586E .
RH41 SNV: p.N1032S .

Probe(s) Labeling This Target

ABPP Probe
Click To Hide/Show 1 Probe Related to This Target
Probe name Structure Binding Site(Ratio) Interaction ID Ref
NAIA_5
 Probe Info  		C556(20.00)  LDD2227  [1]

Competitor(s) Related to This Target

Competitor ID Name Cell line Binding Site(Ratio) Interaction ID Ref
 LDCM0632  CL-Sc Hep-G2 C556(20.00)  LDD2227  [1]

References

1 N-Acryloylindole-alkyne (NAIA) enables imaging and profiling new ligandable cysteines and oxidized thiols by chemoproteomics. Nat Commun. 2023 Jun 15;14(1):3564. doi: 10.1038/s41467-023-39268-w.
Mass spectrometry data entry: PXD041264