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

PRKG2 (Q13237) - Overview - Molecular Target Synopsis

Protein


PRKG2, cGMP-dependent protein kinase 2
Enzyme Classification 2.7.11.12
UniProt Q13237

Also Known as KGP2_HUMAN, PRKG2, PRKGR2

Crucial regulator of intestinal secretion and bone growth (By similarity). Phosphorylates and activates CFTR on the plasma membrane. Plays a key role in intestinal secretion by regulating cGMP-dependent translocation of CFTR in jejunum (By similarity). Acts downstream of NMDAR to activate the plasma membrane accumulation of GRIA1/GLUR1 in synapse and increase synaptic plasticity. Phosphorylates GRIA1/GLUR1 at Ser-863 (By similarity). Acts as regulator of gene expression and activator of the extracellular signal-regulated kinases MAPK3/ERK1 and MAPK1/ERK2 in mechanically stimulated osteoblasts. Under fluid shear stress, mediates ERK activation and subsequent induction of FOS, FOSL1/FRA1, FOSL2/FRA2 and FOSB that play a key role in the osteoblast anabolic response to mechanical stimulation. Interacts with GRIA1/GLUR1.

6BQ8
JOINT X-RAY/NEUTRON STRUCTURE OF PKG II CNB-B DOMAIN IN COMPLEX WITH 8-PCPT-CGMP
RCSB/PDB
Inspect Structure
See all 3D Structures for PRKG2

Isoforms / Transcripts (Protein Coding)


Sub-cellular localization


UniProt: PRKG2 is active in the following subcellular-locations: apical cell membrane.
GO terms: PRKG2 is active in the following subcellular-locations: apical plasma membrane, cytosol, nuclear membrane.



UniProt
GO terms

Gene Copy Number Variation


In COSMIC - Cell Lines Project PRKG2 has gain in 0 cell-lines, loss in 1 cell-lines and no signal in 1004 cell-lines. (see details)

Gene Expression


In NCI60, the highest expressing cell lines are: MCF7, HL_60, RPMI_8226

In Array Express (RNA-seq of 675 commonly used human cancer cell lines), the highest expressing cell lines are: NCI-H2106, HCC33, RKN

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: hMSC-AT, SK-N-SH, HSMM

(see details)

RNA Interference


PRKG2 was reported in the following RNAI studies:

Cell - Large Scale Profiling of Kinase Dependencies in Cancer Cell Lines, the highest RNAi cell lines are: MDAMB453, BXPC3. (see details)

3D Structures


For PRKG2 there are:
6 structures (12 chains) solved
6 are solved in complex with at least one small molecule ligand



(see details)
Molecular Target 3D Synopsis

Screening and Chemistry


PRKG2 has been screened with 489 compounds (908 bioactivities), 8 compounds have bioactivities that show binding affinity of <= 500nM (12 bioactivities). (see details)