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

PRKACG (P22612) - Overview - Molecular Target Synopsis

Protein


PRKACG, cAMP-dependent protein kinase catalytic subunit gamma
Enzyme Classification 2.7.11.11
UniProt P22612

Also Known as KAPCG_HUMAN, PRKACG

Phosphorylates a large number of substrates in the cytoplasm and the nucleus. A number of inactive tetrameric holoenzymes are produced by the combination of homo- or heterodimers of the different regulatory subunits associated with two catalytic subunits. cAMP causes the dissociation of the inactive holoenzyme into a dimer of regulatory subunits bound to four cAMP and two free monomeric catalytic subunits.

Isoforms / Transcripts (Protein Coding)


Protein Length Ensembl Gene Ensembl Transcript Ensembl Protein Uniprot Isoform
367ENSG00000165059ENST00000377276ENSP00000366488
351P22612-1

Sub-cellular localization


GO terms: PRKACG is active in the following subcellular-locations: ciliary base, cytosol, intercellular bridge, nucleoplasm.



UniProt
GO terms

Gene Copy Number Variation


In COSMIC - Cell Lines Project PRKACG has gain in 1 cell-lines, loss in 4 cell-lines and no signal in 999 cell-lines. (see details)

Gene Expression


In NCI60, the highest expressing cell lines are: MCF7, SK_OV_3, EKVX

In Array Express (RNA-seq of 675 commonly used human cancer cell lines), the highest expressing cell lines are: Hs 746T, NCI-H209, LN-18

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


PRKACG was reported in the following RNAI studies:

Cell - Large Scale Profiling of Kinase Dependencies in Cancer Cell Lines, the highest RNAi cell lines are: OVISE, SKGT4. (see details)

3D Structures


At greater than 75% identity similarity to PRKACG there are:
224 structures (250 chains) solved
201 are solved in complex with at least one small molecule ligand
4 are solved with an approved drug

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

AMP/ADENOSINE PHOSPHATE (6EH2_A, 6ESA_A),
IPH/PHENOL (3NX8_A),
NCA/NIACINAMIDE (5N3H_A).

(see details)
Molecular Target 3D Synopsis

Screening and Chemistry


PRKACG has been screened with 791 compounds (870 bioactivities), 84 compounds have bioactivities that show binding affinity of <= 500nM (103 bioactivities). (see details)