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TargetEnzymes

Serine/threonine-protein kinase BRSK2

Named enzymes, including the metabolising cytochromes and the monoamine oxidases.

Measurements
4
Compounds
4
Binding constants
0
Median pX
—

I · Identity

What this target is

Its function as UniProt states it, where in a cell the protein is found, and which cell types and tissues transcribe its gene.

Protein

BRSK2_HUMANBRSK2Homo sapiens

Serine/threonine-protein kinase BRSK2

Serine/threonine-protein kinase that plays a key role in polarization of neurons and axonogenesis, cell cycle progress and insulin secretion. Phosphorylates CDK16, CDC25C, MAPT/TAU, PAK1 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. Plays a role in the regulation of the mitotic cell cycle progress and the onset of mitosis. Plays a role in the regulation of insulin secretion in response to elevated glucose levels, probably via phosphorylation of CDK16 and PAK1. While BRSK2 phosphorylated at Thr-174 can inhibit insulin secretion22798068, BRSK2 phosphorylated at Thr-260 can promote insulin secretion22669945. Regulates reorganization of the actin cytoskeleton. May play a role in the apoptotic response triggered by endoplasmic reticulum (ER) stress

Quoted from UniProt’s FUNCTION annotation for Q8IWQ3 (reviewed). The superscript numbers are UniProt’s own PubMed citations, kept in the sentence and in order, each linking to the paper it names.

What it acts with

STRING’s highest-confidence human functional partners. The combined score mixes several kinds of evidence, so each channel is shown separately — a partner supported by experiment is a different claim from one supported only by text mining, and for a receptor this is where its coupling appears as evidence rather than as assertion.

PartnerCombinedExperimentDatabaseText mining
CDC25B0.8150.6190.0000.533
CDC25C0.7770.6190.0000.439
WEE10.7430.5830.0000.370
CDR20.5710.0000.0000.571
TSC20.5690.0000.0000.563
CDC25A0.5640.4850.0000.187
TSC10.5520.0000.0000.552
PKMYT10.5520.4360.0000.190
PKD10.5470.0000.0000.497
WEE20.5450.4360.0000.178

Where it sits in the cell

  • Golgi apparatus

Human Protein Atlas, by antibody immunofluorescence in cell lines — a different assay from the expression figures below, which are RNA.

UniProt, curated Cytoplasm, cytoskeleton, microtubule organizing center, centrosome · Cytoplasm, perinuclear region · Endoplasmic reticulum

Expression by cell type

Single cell type RNA, the 12 highest of those the Human Protein Atlas reports for this gene. Transcript, not protein, and a cell type rather than a tissue.

  • Retinal bipolar cells67.9 nCPM
  • Brain excitatory neurons61.6 nCPM
  • Pancreatic acinar cells47.1 nCPM
  • Brain inhibitory neurons46.8 nCPM
  • Retinal amacrine cells45.5 nCPM
  • Oligodendrocyte progenitor cells44.6 nCPM
  • Retinal horizontal cells42.1 nCPM
  • Other brain neurons40.6 nCPM
  • Vascular smooth muscle cells39.6 nCPM
  • Gonadotrophs35.9 nCPM
  • Oligodendrocytes34.2 nCPM
  • Sertoli cells32.2 nCPM

Expression by tissue

The tissues this gene is enriched in, by consensus RNA. A tissue absent from this list is one the Atlas does not call specific for this gene, which is not the same as absent from it.

  • pancreas97 nTPM
  • brain96.9 nTPM

IV · Evidence

Every measurement at this target

Each row links to the ChEMBL assay it came from.

Other measurements 4

Everything else ChEMBL recorded for this compound — percentage inhibition, efficacy, half-life, cytotoxicity. Reported in the assay's own units, which is why no value is converted here.

TargetClassTypeValue (nM)pXOrganismAssay
Serine/threonine-protein kinase BRSK2EnzymesActivity— no normalized value— value does not convert to pXHomo sapiensCHEMBL1051367
Serine/threonine-protein kinase BRSK2EnzymesActivity— no normalized value— value does not convert to pXHomo sapiensCHEMBL1051367
Serine/threonine-protein kinase BRSK2EnzymesActivity— no normalized value— value does not convert to pXHomo sapiensCHEMBL1051367
Serine/threonine-protein kinase BRSK2EnzymesActivity— no normalized value— value does not convert to pXHomo sapiensCHEMBL1051367