Details of the Target

General Information of Target

Target ID LDTP14022
Target Name Dual specificity tyrosine-phosphorylation-regulated kinase 1B (DYRK1B)
Gene Name DYRK1B
Gene ID 9149
Synonyms
MIRK; Dual specificity tyrosine-phosphorylation-regulated kinase 1B; EC 2.7.12.1; Minibrain-related kinase; Mirk protein kinase
3D Structure
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2D Sequence (FASTA)
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3D Structure (PDB)
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Sequence
MDSGGGSLGLHTPDSRMAHTMIMQDFVAGMAGTAHIDGDHIVVSVPEAVLVSDVVTDDGI
TLDHGLAAEVVHGPDIITETDVVTEGVIVPEAVLEADVAIEEDLEEDDGDHILTSELITE
TVRVPEQVFVADLVTGPNGHLEHVVQDCVSGVDSPTMVSEEVLVTNSDTETVIQAAGGVP
GSTVTIKTEDDDDDDVKSTSEDYLMISLDDVGEKLEHMGNTPLKIGSDGSQEDAKEDGFG
SEVIKVYIFKAEAEDDVEIGGTEIVTESEYTSGHSVAGVLDQSRMQREKMVYMAVKDSSQ
EEDDIRDERRVSRRYEDCQASGNTLDSALESRSSTAAQYLQICDGINTNKVLKQKAKKRR
RGETRQWQTAVIIGPDGQPLTVYPCHICTKKFKSRGFLKRHMKNHPDHLMRKKYQCTDCD
FTTNKKVSFHNHLESHKLINKVDKTHEFTEYTRRYREASPLSSNKLILRDKEPKMHKCKY
CDYETAEQGLLNRHLLAVHSKNFPHVCVECGKGFRHPSELKKHMRTHTGEKPYQCQYCIF
RCADQSNLKTHIKSKHGNNLPYKCEHCPQAFGDERELQRHLDLFQGHKTHQCPHCDHKST
NSSDLKRHIISVHTKDFPHKCEVCDKGFHRPSELKKHSDIHKGRKIHQCRHCDFKTSDPF
ILSGHILSVHTKDQPLKCKRCKRGFRQQNELKKHMKTHTGRKIYQCEYCEYSTTDASGFK
RHVISIHTKDYPHRCEFCKKGFRRPSEKNQHIMRHHKEALM
Target Type
Patented-recorded
Target Bioclass
Enzyme
Family
Protein kinase superfamily, CMGC Ser/Thr protein kinase family, MNB/DYRK subfamily
Subcellular location
Nucleus
Function
Dual-specificity kinase which possesses both serine/threonine and tyrosine kinase activities. Plays an essential role in ribosomal DNA (rDNA) double-strand break repair and rDNA copy number maintenance. During DNA damage, mediates transcription silencing in part via phosphorylating and enforcing DSB accumulation of the histone methyltransferase EHMT2. Enhances the transcriptional activity of TCF1/HNF1A and FOXO1. Inhibits epithelial cell migration. Mediates colon carcinoma cell survival in mitogen-poor environments. Inhibits the SHH and WNT1 pathways, thereby enhancing adipogenesis. In addition, promotes expression of the gluconeogenic enzyme glucose-6-phosphatase catalytic subunit 1 (G6PC1).
TTD ID
T82720
Uniprot ID
Q9Y463
DrugMap ID
TTYGQ8A
Ensemble ID
ENST00000323039.10
HGNC ID
HGNC:3092
ChEMBL ID
CHEMBL5543

Target Site Mutations in Different Cell Lines

Cell line Mutation details Probe for labeling this protein in this cell
HCT15 SNV: p.Q511Ter .
HT115 SNV: p.E18D .
ICC10 SNV: p.R547P .
JURKAT SNV: p.S314N .
NCIH196 SNV: p.C264R DBIA    Probe Info 
NCIH23 SNV: p.K345N .
OVK18 SNV: p.T308N .
SG231 SNV: p.Q72L .
SNU449 SNV: p.R359K .
SUPT1 SNV: p.Q72P DBIA    Probe Info 
YSCCC SNV: p.E393K .

Probe(s) Labeling This Target

ABPP Probe
Click To Hide/Show 3 Probe Related to This Target
Probe name Structure Binding Site(Ratio) Interaction ID Ref
m-APA
 Probe Info  		15.00  LDD0402  [1]
DBIA
 Probe Info  		C312(3.64)  LDD3334  [2]
IA-alkyne
 Probe Info  		N.A.  LDD0162  [3]

Competitor(s) Related to This Target

Competitor ID Name Cell line Binding Site(Ratio) Interaction ID Ref
 LDCM0022  KB02 697 C312(5.15)  LDD2245  [2]
 LDCM0023  KB03 697 C312(9.15)  LDD2662  [2]
 LDCM0024  KB05 MOLM-16 C312(3.64)  LDD3334  [2]

The Interaction Atlas With This Target

The Protein(s) Related To This Target

Enzyme
Click To Hide/Show 2 Protein(s) Interacting with This Target
Protein name Family Uniprot ID
Dual specificity mitogen-activated protein kinase kinase 3 (MAP2K3) STE Ser/Thr protein kinase family P46734
Pterin-4-alpha-carbinolamine dehydratase 2 (PCBD2) Pterin-4-alpha-carbinolamine dehydratase family Q9H0N5
Transporter and channel
Click To Hide/Show 1 Protein(s) Interacting with This Target
Protein name Family Uniprot ID
Heat shock protein HSP 90-beta (HSP90AB1) Heat shock protein 90 family P08238
Transcription factor
Click To Hide/Show 2 Protein(s) Interacting with This Target
Protein name Family Uniprot ID
Hepatocyte nuclear factor 1-alpha (HNF1A) HNF1 homeobox family P20823
Homeobox protein goosecoid-2 (GSC2) Paired homeobox family O15499
Other
Click To Hide/Show 6 Protein(s) Interacting with This Target
Protein name Family Uniprot ID
Leucine zipper putative tumor suppressor 2 (LZTS2) LZTS2 family Q9BRK4
Ran-binding protein 9 (RANBP9) RANBP9/10 family Q96S59
Retinoblastoma-associated protein (RB1) Retinoblastoma protein (RB) family P06400
Retinoblastoma-like protein 1 (RBL1) Retinoblastoma protein (RB) family P28749
DDB1- and CUL4-associated factor 7 (DCAF7) WD repeat DCAF7 family P61962
Tastin (TROAP) . Q12815

The Drug(s) Related To This Target

Approved
Click To Hide/Show 1 Drug(s) Interacting with This Target
Drug Name Drug Type External ID
Fostamatinib Small molecular drug DB12010
Investigative
Click To Hide/Show 3 Drug(s) Interacting with This Target
Drug Name Drug Type External ID
Pmid23642479c17 Small molecular drug D06CXU
Pmid24900699c68 Small molecular drug D0X9PI
Wo2013026806c72 Small molecular drug D00AQR
Patented
Click To Hide/Show 18 Drug(s) Interacting with This Target
Drug Name Drug Type External ID
Pmid28766366-compound-scheme14bindy Small molecular drug D04SYJ
Pmid28766366-compound-scheme21left Small molecular drug D02DBH
Pmid28766366-compound-scheme21right Small molecular drug D07BWC
Pmid28766366-compound-scheme25-2 Small molecular drug D09CDR
Pmid28766366-compound-scheme25-3 Small molecular drug D0CC7E
Pmid28766366-compound-scheme25-4 Small molecular drug D0GE4F
Pmid28766366-compound-scheme4bottom Small molecular drug D0SB1W
Pmid28766366-compound-scheme4upper Small molecular drug D0C0BP
Pmid28766366-compound-scheme5 Small molecular drug D0P7QO
Pmid28766366-compound-scheme9eht1610 Small molecular drug D08CUF
Pmid28766366-compound-scheme9eht3356 Small molecular drug D0DT5I
Pmid28766366-compound-scheme9eht5372 Small molecular drug D08DIJ
Pmid28766366-compound-scheme9eht6840 Small molecular drug D0O9BK
Pmid28766366-compound-scheme9eht9851 Small molecular drug D0PJ1W
Pmid28766366-compound-scheme2wo2012/098065bottom . D00TFF
Pmid28766366-compound-scheme2wo2012/098065upper . D0B8IQ
Pmid28766366-compound-scheme7wo2012/098070bottom . D0BP6J
Pmid28766366-compound-scheme7wo2012/098070upper . D05CLL

References

1 Quantitative and Site-Specific Chemoproteomic Profiling of Targets of Acrolein. Chem Res Toxicol. 2019 Mar 18;32(3):467-473. doi: 10.1021/acs.chemrestox.8b00343. Epub 2019 Jan 15.
2 DrugMap: A quantitative pan-cancer analysis of cysteine ligandability. Cell. 2024 May 9;187(10):2536-2556.e30. doi: 10.1016/j.cell.2024.03.027. Epub 2024 Apr 22.
Mass spectrometry data entry: PXD047840
3 SP3-FAIMS Chemoproteomics for High-Coverage Profiling of the Human Cysteinome*. Chembiochem. 2021 May 14;22(10):1841-1851. doi: 10.1002/cbic.202000870. Epub 2021 Feb 18.
Mass spectrometry data entry: PXD023056 , PXD023059 , PXD023058 , PXD023057 , PXD023060