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

GRK1 (Q15835) - Overview - Molecular Target Synopsis

Protein


GRK1, Rhodopsin kinase
Enzyme Classification 2.7.11.14
UniProt Q15835

Also Known as RK_HUMAN, GRK1, RHOK

Retina-specific kinase involved in the signal turnoff via phosphorylation of rhodopsin (RHO), the G protein- coupled receptor that initiates the phototransduction cascade. This rapid desensitization is essential for scotopic vision and permits rapid adaptation to changes in illumination. Interacts (when prenylated) with PDE6D; this promotes release from membranes.

5AFP
12 RESIDUE FRAGMENT OF
RHODOPSIN KINASE
IN THE STRUCTURE OF
NEURONAL CALCIUM SENSOR-1 (NCS-1)FROM RATTUS NORVEGICUS COMPLEX WITH RHODOPSIN KINASE PEPTIDE FROM HOMO SAPIENS
RCSB/PDB
Inspect Structure
See all 3D Structures for GRK1

Isoforms / Transcripts (Protein Coding)


Protein Length Ensembl Gene Ensembl Transcript Ensembl Protein Uniprot Isoform
563ENSG00000185974ENST00000335678ENSP00000334876Q15835-1

Sub-cellular localization


UniProt: GRK1 is active in the following subcellular-locations: membrane.
GO terms: GRK1 is active in the following subcellular-locations: photoreceptor disc membrane.



UniProt
GO terms

Gene Copy Number Variation


In COSMIC - Cell Lines Project GRK1 has gain in 2 cell-lines, loss in 7 cell-lines and no signal in 996 cell-lines. (see details)

Gene Expression


In NCI60, the highest expressing cell lines are: MCF7, LOXIMVI, NCI_H460

In Array Express (RNA-seq of 675 commonly used human cancer cell lines), the highest expressing cell lines are: DMS 79, NCI-H345, LNCAP

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


GRK1 was reported in the following RNAI studies:

Cell - Large Scale Profiling of Kinase Dependencies in Cancer Cell Lines, the highest RNAi cell lines are: SKGT4, MCF12A. (see details)

3D Structures


For GRK1 there are:
1 structures (2 chains) solved
0 are solved in complex with at least one small molecule ligand



(see details)
Molecular Target 3D Synopsis

Screening and Chemistry


GRK1 has been screened with 121 compounds (128 bioactivities), 8 compounds have bioactivities that show binding affinity of <= 500nM (11 bioactivities). (see details)