Molecular Target Synopsis
Domains and Structures
Drugs and Clinical Candidates
Ligand Efficiency Plot
Family Cladogram
Interaction Network
Gene Expression
Gene Copy Number Variation
Germline Genetics

BRSK2 (Q8IWQ3) - Overview - Molecular Target Synopsis


BRSK2, Serine/threonine-protein kinase BRSK2
Enzyme Classification
UniProt Q8IWQ3

Also Known as BRSK2_HUMAN, BRSK2, C11orf7, PEN11B, SADA, STK29

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 secretion (PubMed:22798068), BRSK2 phosphorylated at Thr-260 can promote insulin secretion (PubMed:22669945). Regulates reorganization of the actin cytoskeleton. May play a role in the apoptotic response triggered by endoplasmic reticulum (ER) stress. Interacts with FZR1, a regulatory subunit of the APC ubiquitin ligase complex. Interacts with COPS5. Interacts with PAK1.

Isoforms / Transcripts (Protein Coding)

Sub-cellular localization

UniProt: BRSK2 is active in the following subcellular-locations: centrosome, cytoplasm, cytoskeleton, endoplasmic reticulum, microtubule organizing center, perinuclear region.
GO terms: BRSK2 is active in the following subcellular-locations: centrosome, cytoplasm, distal axon, endoplasmic reticulum, nucleus, perinuclear region of cytoplasm.

GO terms

Gene Copy Number Variation

In COSMIC - Cell Lines Project BRSK2 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: NCI_H522, UACC_257, HCT_116

In Array Express (RNA-seq of 675 commonly used human cancer cell lines), the highest expressing cell lines are: SCLC-21H, NCI-H1930, NCI-H446

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: SK-N-SH, NHLF, HSMM

(see details)

RNA Interference

BRSK2 was reported in the following RNAI studies:

Cell - Large Scale Profiling of Kinase Dependencies in Cancer Cell Lines, the highest RNAi cell lines are: SKGT4, JIMT1. (see details)

3D Structures

At greater than 90% identity similarity to BRSK2 there are:
2 structures (4 chains) solved
0 are solved in complex with at least one small molecule ligand

(see details)
Molecular Target 3D Synopsis

Screening and Chemistry

BRSK2 has been screened with 752 compounds (1377 bioactivities), 6 compounds have bioactivities that show binding affinity of <= 500nM (8 bioactivities). (see details)