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

AKT3 (Q9Y243) - Overview - Molecular Target Synopsis

Protein


AKT3, RAC-gamma serine/threonine-protein kinase
Enzyme Classification 2.7.11.1
UniProt Q9Y243

Also Known as AKT3_HUMAN, AKT3, PKBG

AKT3 is one of 3 closely related serine/threonine-protein kinases (AKT1, AKT2 and AKT3) called the AKT kinase, and which regulate many processes including metabolism, proliferation, cell survival, growth and angiogenesis. This is mediated through serine and/or threonine phosphorylation of a range of downstream substrates. Over 100 substrate candidates have been reported so far, but for most of them, no isoform specificity has been reported. AKT3 is the least studied AKT isoform. It plays an important role in brain development and is crucial for the viability of malignant glioma cells. AKT3 isoform may also be the key molecule in up-regulation and down-regulation of MMP13 via IL13. Required for the coordination of mitochondrial biogenesis with growth factor-induced increases in cellular energy demands. Down-regulation by RNA interference reduces the expression of the phosphorylated form of BAD, resulting in the induction of caspase-dependent apoptosis. Interacts (via PH domain) with TCL1A; this enhances AKT3 phosphorylation and activation. Interacts with TRAF6. Interacts with KCTD20 (By similarity). Interacts with BTBD10.

2X18
THE CRYSTAL STRUCTURE OF THE PH DOMAIN OF HUMAN AKT3 PROTEIN KINASE
RCSB/PDB
Inspect Structure
See all 3D Structures for AKT3

Isoforms / Transcripts (Protein Coding)


Sub-cellular localization


UniProt: AKT3 is active in the following subcellular-locations: cytoplasm, membrane, nucleus.
GO terms: AKT3 is active in the following subcellular-locations: cytoplasm, membrane, nucleus.



UniProt
GO terms

Gene Copy Number Variation


In COSMIC - Cell Lines Project AKT3 has gain in 5 cell-lines, loss in 1 cell-lines and no signal in 999 cell-lines. (see details)

Gene Expression


In NCI60, the highest expressing cell lines are: HS578T, SN12C, CAKI_1

In Array Express (RNA-seq of 675 commonly used human cancer cell lines), the highest expressing cell lines are: NCI-H209, CAL-120, NCI-H2804

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: NHLF, BJ, SK-N-SH

(see details)

RNA Interference


AKT3 was reported in the following RNAI studies:

Cell - Large Scale Profiling of Kinase Dependencies in Cancer Cell Lines, the highest RNAi cell lines are: COV362, H1838. (see details)

3D Structures


For AKT3 there are:
1 structures (8 chains) solved
1 are solved in complex with at least one small molecule ligand



(see details)
Molecular Target 3D Synopsis

Screening and Chemistry


AKT3 has been screened with 1045 compounds (1787 bioactivities), 134 compounds have bioactivities that show binding affinity of <= 500nM (170 bioactivities). (see details)