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

CAMK2A (Q9UQM7) - Overview - Molecular Target Synopsis

Protein


CAMK2A, Calcium/calmodulin-dependent protein kinase type II subunit alpha
Enzyme Classification 2.7.11.17
UniProt Q9UQM7

Also Known as KCC2A_HUMAN, CAMK2A, CAMKA, KIAA0968

Calcium/calmodulin-dependent protein kinase that functions autonomously after Ca(2+)/calmodulin-binding and autophosphorylation, and is involved in synaptic plasticity, neurotransmitter release and long-term potentiation. Member of the NMDAR signaling complex in excitatory synapses, it regulates NMDAR-dependent potentiation of the AMPAR and therefore excitatory synaptic transmission (By similarity). Regulates dendritic spine development (PubMed:28130356). Also regulates the migration of developing neurons (PubMed:29100089). Phosphorylates the transcription factor FOXO3 to activate its transcriptional activity (PubMed:23805378). There are 4 genes encoding calcium/calmodulin-dependent protein kinase type II chains: CAMK2A, CAMK2B, CAMK2G and CAMK2D. The corresponding proteins assemble into homo- or heteromultimeric holoenzymes composed of 12 subunits with two hexameric rings stacked one on top of the other (PubMed:14722083, PubMed:29784083). Interacts with BAALC. Interacts with MPDZ. Interacts with SYN1. Interacts with CAMK2N2. Interacts with SYNGAP1. Interacts with SYNPO2 (By similarity). Interacts with SHANK3 (PubMed:28130356). Interacts with GRIN2B (PubMed:28130356). Interacts with CACNB2 (PubMed:28130356). Interacts with LRRC7 (PubMed:28130356). Interacts with GRM5 (PubMed:28130356).

6OF8
STRUCTURE OF THR354ASN, GLU355GLN, THR412ASN, ILE414MET, ILE464HIS, AND PHE467MET MUTANT HUMAN CAMKII-ALPHA HUB DOMAIN
RCSB/PDB
Inspect Structure
See all 3D Structures for CAMK2A

Isoforms / Transcripts (Protein Coding)


Sub-cellular localization


UniProt: CAMK2A is active in the following subcellular-locations: cell junction, cell projection, dendrite, dendritic spine, postsynaptic cell membrane, postsynaptic density, synapse.
GO terms: CAMK2A is active in the following subcellular-locations: calcium- and calmodulin-dependent protein kinase complex, cell junction, cytoplasm, cytosol, dendritic spine, endocytic vesicle membrane, mitochondrion, neuron projection, nucleoplasm, nucleus, plasma membrane, postsynaptic density, postsynaptic membrane, Schaffer collateral - CA1 synapse.



UniProt
GO terms

Gene Copy Number Variation


In COSMIC - Cell Lines Project CAMK2A has gain in 1 cell-lines, loss in 1 cell-lines and no signal in 1003 cell-lines. (see details)

Gene Expression


In NCI60, the highest expressing cell lines are: SN12C, UACC_62, PC_3

In Array Express (RNA-seq of 675 commonly used human cancer cell lines), the highest expressing cell lines are: NCI-H226, NCI-H2596, SNU-182

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, HMEC

(see details)

RNA Interference


CAMK2A was reported in the following RNAI studies:

Cell - Large Scale Profiling of Kinase Dependencies in Cancer Cell Lines, the highest RNAi cell lines are: G292, MG63. (see details)

3D Structures


For CAMK2A there are:
6 structures (42 chains) solved
3 are solved in complex with at least one small molecule ligand
1 are solved with an approved drug

CAMK2A is solved in complex with the approved drug(s):

DB8/BOSUTINIB (3SOA_A).

(see details)
Molecular Target 3D Synopsis

Screening and Chemistry


CAMK2A has been screened with 950 compounds (1435 bioactivities), 35 compounds have bioactivities that show binding affinity of <= 500nM (49 bioactivities). (see details)