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

CAMK2A (Q9UQM7) - Overview - Molecular Target Synopsis


CAMK2A, Calcium/calmodulin-dependent protein kinase type II subunit alpha
Enzyme Classification
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).

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.

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:
5 structures (35 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):


(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)