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

GRK7 (Q8WTQ7) - Overview - Molecular Target Synopsis

Protein


GRK7, Rhodopsin kinase
Enzyme Classification 2.7.11.14
UniProt Q8WTQ7

Also Known as GRK7_HUMAN, GRK7, GPRK7

Retina-specific kinase involved in the shutoff of the photoresponse and adaptation to changing light conditions via cone opsin phosphorylation, including rhodopsin (RHO). Interacts (when prenylated) with PDE6D; this promotes release from membranes.

Isoforms / Transcripts (Protein Coding)


Protein Length Ensembl Gene Ensembl Transcript Ensembl Protein Uniprot Isoform
553ENSG00000114124ENST00000264952ENSP00000264952Q8WTQ7-1

Sub-cellular localization


UniProt: GRK7 is active in the following subcellular-locations: membrane.
GO terms: GRK7 is active in the following subcellular-locations: photoreceptor disc membrane.



UniProt
GO terms

Gene Copy Number Variation


In COSMIC - Cell Lines Project GRK7 has gain in 2 cell-lines, loss in 1 cell-lines and no signal in 1002 cell-lines. (see details)

Gene Expression


In NCI60, the highest expressing cell lines are:

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


GRK7 was reported in the following RNAI studies:

Cell - Large Scale Profiling of Kinase Dependencies in Cancer Cell Lines, the highest RNAi cell lines are: HCC1954, SCC90. (see details)

3D Structures


At greater than 35% identity similarity to GRK7 there are:
67 structures (98 chains) solved
60 are solved in complex with at least one small molecule ligand
3 are solved with an approved drug

GRK7 is solved in complex with the approved drug(s):

ANW/AMLEXANOX (4WBO_A, 4WBO_B, 4WBO_C, 4WBO_D),
AMP/ADENOSINE PHOSPHATE (3NYO_A, 3NYO_B),
8PR/PAROXETINE (4L9I_A, 4L9I_B).

(see details)
Molecular Target 3D Synopsis

Screening and Chemistry


GRK7 has been screened with 633 compounds (1178 bioactivities), 10 compounds have bioactivities that show binding affinity of <= 500nM (13 bioactivities). (see details)