Tbio ARHGEF2 Rho guanine nucleotide exchange factor 2

Protein Summary

Description

Activates Rho-GTPases by promoting the exchange of GDP for GTP. May be involved in epithelial barrier permeability, cell motility and polarization, dendritic spine morphology, antigen presentation, leukemic cell differentiation, cell cycle regulation, innate immune response, and cancer. Binds Rac-GTPases, but does not seem to promote nucleotide exchange activity toward Rac-GTPases, which was uniquely reported in PubMed:9857026. May stimulate instead the cortical activity of Rac. Inactive toward CDC42, TC10, or Ras-GTPases. Forms an intracellular sensing system along with NOD1 for the detection of microbial effectors during cell invasion by pathogens. Required for RHOA and RIP2 dependent NF-kappaB signaling pathways activation upon S.flexneri cell invasion. Involved not only in sensing peptidoglycan (PGN)-derived muropeptides through NOD1 that is independent of its GEF activity, but also in the activation of NF-kappaB by Shigella effector proteins (IpgB2 and OspB) which requires its GEF activity and the activation of RhoA. Involved in innate immune signaling transduction pathway promoting cytokine IL6/interleukin-6 and TNF-alpha secretion in macrophage upon stimulation by bacterial peptidoglycans; acts as a signaling intermediate between NOD2 receptor and RIPK2 kinase. Contributes to the tyrosine phosphorylation of RIPK2 through Src tyrosine kinase leading to NF-kappaB activation by NOD2. Overexpression activates Rho-, but not Rac-GTPases, and increases paracellular permeability (By similarity). Involved in neuronal progenitor cell division and differentiation (PubMed:28453519). Involved in the migration of precerebellar neurons (By similarity). Rho GTPases play a fundamental role in numerous cellular processes that are initiated by extracellular stimuli that work through G protein coupled receptors. The encoded protein may form complex with G proteins and stimulate rho-dependent signals. Alternatively spliced transcript variants encoding different isoforms have been identified.[provided by RefSeq, Jun 2009]

Uniprot Accession IDs

• Q92974
• D3DVA6
• O75142
• Q15079
• Q5VY92
• Q8TDA3
• Q8WUG4
• Q9H023

Gene Name

• ARHGEF2

Ensembl ID

• ENST00000313667
• ENSP00000314787
• ENSG00000116584
• ENST00000313695
• ENSP00000315325
• ENST00000361247
• ENSP00000354837

Symbol

• KIAA0651
• LFP40
• GEF
• P40
• GEFH1
• LFP40
• GEF-H1
• NEDMHM

Knowledge Table

Most Knowledge About	Knowledge Value (0 to 1 scale)
biological process	1
drug perturbation	1
interacting protein	1
protein complex	1
transcription factor perturbation	0.98

Protein Classes

DTO Classes

Rho Guanine Nucleotide Exchange Factor 25

IDG Development Level Summary

Tdark

These are targets about which virtually nothing is known. They do not have known drug or small molecule activities
- AND - satisfy two or more of the following criteria:

Pubmed score: 95.35   (req: < 5)

Gene RIFs: 54   (req: <= 3)

Antibodies: 398   (req: <= 50)

Tbio

These targets do not have known drug or small molecule activities
- AND - satisfy two or more of the following criteria:

Pubmed score: 95.35   (req: >= 5)

Gene RIFs: 54   (req: > 3)

Antibodies: 398   (req: > 50)

- OR - satisfy the following criterion:

Gene Ontology Terms: 36

Tchem

Target has at least one ChEMBL compound with an activity cutoff of < 30 nM - AND - satisfies the preceding conditions

Active Ligand: 0

Tclin

Target has at least one approved drug - AND - satisfies the preceding conditions

Active Drug: 0