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

CSNK1G2 (P78368) - Overview - Molecular Target Synopsis

Protein


CSNK1G2, Casein kinase I isoform gamma-2
Enzyme Classification 2.7.11.1
UniProt P78368

Also Known as KC1G2_HUMAN, CSNK1G2, CK1G2

Serine/threonine-protein kinase. Casein kinases are operationally defined by their preferential utilization of acidic proteins such as caseins as substrates. It can phosphorylate a large number of proteins. Participates in Wnt signaling. Phosphorylates COL4A3BP/CERT, MTA1 and SMAD3. Involved in brain development and vesicular trafficking and neurotransmitter releasing from small synaptic vesicles. Regulates fast synaptic transmission mediated by glutamate. SMAD3 phosphorylation promotes its ligand-dependent ubiquitination and subsequent proteasome degradation, thus inhibiting SMAD3-mediated TGF-beta responses. Hyperphosphorylation of the serine-repeat motif of COL4A3BP/CERT leads to its inactivation by dissociation from the Golgi complex, thus down-regulating ER-to-Golgi transport of ceramide and sphingomyelin synthesis. Triggers PER1 proteasomal degradation probably through phosphorylation. Monomer (By similarity). Interacts with MTA1 (short isoform) in the cytoplasm. Interacts with SMAD3.

2C47
STRUCTURE OF CASEIN KINASE 1 GAMMA 2
RCSB/PDB
Inspect Structure
See all 3D Structures for CSNK1G2

Isoforms / Transcripts (Protein Coding)


Sub-cellular localization


UniProt: CSNK1G2 is active in the following subcellular-locations: cytoplasm.
GO terms: CSNK1G2 is active in the following subcellular-locations: cytoplasm, cytosol, membrane, nucleus, plasma membrane.



UniProt
GO terms

Gene Copy Number Variation


In COSMIC - Cell Lines Project CSNK1G2 has gain in 0 cell-lines, loss in 5 cell-lines and no signal in 1000 cell-lines. (see details)

Gene Expression


In NCI60, the highest expressing cell lines are: HL_60, SR, HCT_15

In Array Express (RNA-seq of 675 commonly used human cancer cell lines), the highest expressing cell lines are: Detroit 562, G120, LCLC-97TM1

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, K562, A549

(see details)

RNA Interference


CSNK1G2 was reported in the following RNAI studies:

Cell - Large Scale Profiling of Kinase Dependencies in Cancer Cell Lines, the highest RNAi cell lines are: MIAPACA2, OVTOKO. (see details)

3D Structures


For CSNK1G2 there are:
1 structures (4 chains) solved
1 are solved in complex with at least one small molecule ligand



(see details)
Molecular Target 3D Synopsis

Screening and Chemistry


CSNK1G2 has been screened with 841 compounds (1542 bioactivities), 16 compounds have bioactivities that show binding affinity of <= 500nM (24 bioactivities). (see details)