Details of the Target

General Information of Target

Target ID LDTP09427
Target Name Serine/threonine-protein kinase BRSK1 (BRSK1)
Gene Name BRSK1
Gene ID 84446
Synonyms
KIAA1811; SAD1; SADB; Serine/threonine-protein kinase BRSK1; EC 2.7.11.1; Brain-selective kinase 1; EC 2.7.11.26; Brain-specific serine/threonine-protein kinase 1; BR serine/threonine-protein kinase 1; Serine/threonine-protein kinase SAD-B; Synapses of Amphids Defective homolog 1; SAD1 homolog; hSAD1
3D Structure
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2D Sequence (FASTA)
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3D Structure (PDB)
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Sequence
MSSGAKEGGGGSPAYHLPHPHPHPPQHAQYVGPYRLEKTLGKGQTGLVKLGVHCITGQKV
AIKIVNREKLSESVLMKVEREIAILKLIEHPHVLKLHDVYENKKYLYLVLEHVSGGELFD
YLVKKGRLTPKEARKFFRQIVSALDFCHSYSICHRDLKPENLLLDEKNNIRIADFGMASL
QVGDSLLETSCGSPHYACPEVIKGEKYDGRRADMWSCGVILFALLVGALPFDDDNLRQLL
EKVKRGVFHMPHFIPPDCQSLLRGMIEVEPEKRLSLEQIQKHPWYLGGKHEPDPCLEPAP
GRRVAMRSLPSNGELDPDVLESMASLGCFRDRERLHRELRSEEENQEKMIYYLLLDRKER
YPSCEDQDLPPRNDVDPPRKRVDSPMLSRHGKRRPERKSMEVLSITDAGGGGSPVPTRRA
LEMAQHSQRSRSVSGASTGLSSSPLSSPRSPVFSFSPEPGAGDEARGGGSPTSKTQTLPS
RGPRGGGAGEQPPPPSARSTPLPGPPGSPRSSGGTPLHSPLHTPRASPTGTPGTTPPPSP
GGGVGGAAWRSRLNSIRNSFLGSPRFHRRKMQVPTAEEMSSLTPESSPELAKRSWFGNFI
SLDKEEQIFLVLKDKPLSSIKADIVHAFLSIPSLSHSVLSQTSFRAEYKASGGPSVFQKP
VRFQVDISSSEGPEPSPRRDGSGGGGIYSVTFTLISGPSRRFKRVVETIQAQLLSTHDQP
SVQALADEKNGAQTRPAGAPPRSLQPPPGRPDPELSSSPRRGPPKDKKLLATNGTPLP
Target Type
Literature-reported
Target Bioclass
Enzyme
Family
Protein kinase superfamily, CAMK Ser/Thr protein kinase family, SNF1 subfamily
Subcellular location
Cytoplasm
Function
Serine/threonine-protein kinase that plays a key role in polarization of neurons and centrosome duplication. Phosphorylates CDC25B, CDC25C, MAPT/TAU, RIMS1, TUBG1, TUBG2 and WEE1. Following phosphorylation and activation by STK11/LKB1, acts as a key regulator of polarization of cortical neurons, probably by mediating phosphorylation of microtubule-associated proteins such as MAPT/TAU at 'Thr-529' and 'Ser-579'. Also regulates neuron polarization by mediating phosphorylation of WEE1 at 'Ser-642' in postmitotic neurons, leading to down-regulate WEE1 activity in polarized neurons. In neurons, localizes to synaptic vesicles and plays a role in neurotransmitter release, possibly by phosphorylating RIMS1. Also acts as a positive regulator of centrosome duplication by mediating phosphorylation of gamma-tubulin (TUBG1 and TUBG2) at 'Ser-131', leading to translocation of gamma-tubulin and its associated proteins to the centrosome. Involved in the UV-induced DNA damage checkpoint response, probably by inhibiting CDK1 activity through phosphorylation and activation of WEE1, and inhibition of CDC25B and CDC25C.
TTD ID
T20053
Uniprot ID
Q8TDC3
DrugMap ID
TTV6WMQ
Ensemble ID
ENST00000309383.6
HGNC ID
HGNC:18994
ChEMBL ID
CHEMBL5650

Target Site Mutations in Different Cell Lines

Cell line Mutation details Probe for labeling this protein in this cell
COLO792 SNV: p.R134P .
CORL23 SNV: p.R510P .
HCT116 Deletion: p.P747HfsTer9 .
HEC1B SNV: p.R742Ter .
HT SNV: p.D680G .
HUPT3 SNV: p.P25H .
MEWO SNV: p.P588S .
MFE319 SNV: p.T477M .
MOLT4 SNV: p.E37K
Substitution: p.E458Ter		 .
PATU8988T SNV: p.E166D .
RKO SNV: p.R429I .
RL SNV: p.S71L .
TFK1 SNV: p.R397W .
TKKK SNV: p.S311F .

Probe(s) Labeling This Target

ABPP Probe
Click To Hide/Show 2 Probe Related to This Target
Probe name Structure Binding Site(Ratio) Interaction ID Ref
DBIA
 Probe Info  		C311(1.38)  LDD2469  [1]
ATP probe
 Probe Info  		N.A.  LDD0199  [2]

Competitor(s) Related to This Target

Competitor ID Name Cell line Binding Site(Ratio) Interaction ID Ref
 LDCM0022  KB02 MGG123 C311(1.38)  LDD2469  [1]
 LDCM0023  KB03 MGG123 C311(1.74)  LDD2886  [1]
 LDCM0024  KB05 MGG123 C311(1.83)  LDD3303  [1]

The Interaction Atlas With This Target

The Drug(s) Related To This Target

Investigative
Click To Hide/Show 1 Drug(s) Interacting with This Target
Drug Name Drug Type External ID
Cct244747 Small molecular drug D0Z8PT

References

1 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
2 Targeted Proteomic Approaches for Proteome-Wide Characterizations of the AMP-Binding Capacities of Kinases. J Proteome Res. 2022 Aug 5;21(8):2063-2070. doi: 10.1021/acs.jproteome.2c00225. Epub 2022 Jul 12.