Molecular Target Synopsis
Overview
Domains and Structures
Drugs and Clinical Candidates
Druggability
Chemistry
Ligand Efficiency Plot
Pathways
Family Cladogram
Interaction Network
Gene Expression
Gene Copy Number Variation
RNAi
Mutations
Germline Genetics

BRSK2 (Q8IWQ3) - Overview - Molecular Target Synopsis

Protein


BRSK2, Serine/threonine-protein kinase BRSK2
Enzyme Classification 2.7.11.1
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.



UniProt
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)