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

CDC42BPG (Q6DT37) - Overview - Molecular Target Synopsis

Protein


CDC42BPG, Serine/threonine-protein kinase MRCK gamma
Enzyme Classification 2.7.11.1
UniProt Q6DT37

Also Known as MRCKG_HUMAN, CDC42BPG, DMPK2

May act as a downstream effector of CDC42 in cytoskeletal reorganization. Contributes to the actomyosin contractility required for cell invasion, through the regulation of MYPT1 and thus MLC2 phosphorylation. Homodimer and homotetramer via the coiled coil regions. Interacts tightly with GTP-bound but not GDP-bound CDC42.

Isoforms / Transcripts (Protein Coding)


Protein Length Ensembl Gene Ensembl Transcript Ensembl Protein Uniprot Isoform
1551ENSG00000171219ENST00000342711ENSP00000345133Q6DT37-1

Sub-cellular localization


UniProt: CDC42BPG is active in the following subcellular-locations: cytoplasm.
GO terms: CDC42BPG is active in the following subcellular-locations: cell leading edge, cytosol, microtubule organizing center.



UniProt
GO terms

Gene Copy Number Variation


In COSMIC - Cell Lines Project CDC42BPG has gain in 3 cell-lines, loss in 0 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: BHY, HCC2935, MDA-MB-468

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: K562, MCF-7, SK-N-SH

(see details)

RNA Interference


CDC42BPG was reported in the following RNAI studies:

Cell - Large Scale Profiling of Kinase Dependencies in Cancer Cell Lines, the highest RNAi cell lines are: LM7, RES259. (see details)

3D Structures


At greater than 50% identity similarity to CDC42BPG there are:
31 structures (77 chains) solved
31 are solved in complex with at least one small molecule ligand



(see details)
Molecular Target 3D Synopsis

Screening and Chemistry


CDC42BPG has been screened with 102 compounds (140 bioactivities), 5 compounds have bioactivities that show binding affinity of <= 500nM (7 bioactivities). (see details)