Tbio GPR161 G-protein coupled receptor 161

Protein Summary

Description

Key negative regulator of Shh signaling, which promotes the processing of GLI3 into GLI3R during neural tube development. Recruited by TULP3 and the IFT-A complex to primary cilia and acts as a regulator of the PKA-dependent basal repression machinery in Shh signaling by increasing cAMP levels, leading to promote the PKA-dependent processing of GLI3 into GLI3R and repress the Shh signaling. In presence of SHH, it is removed from primary cilia and is internalized into recycling endosomes, preventing its activity and allowing activation of the Shh signaling. Its ligand is unknown (By similarity). The protein encoded by this gene is an orphan G protein-coupled receptor whose ligand is unknown. This gene is overexpressed in triple-negative breast cancer, and disruption of this gene slows the proliferation of basal breast cancer cells. Therefore, this gene is a potential drug target for triple-negative breast cancer. [provided by RefSeq, Mar 2017]

Uniprot Accession IDs

• Q8N6U8
• B3KV34
• B7Z5D7
• B7Z5E8
• B7Z5Z6
• F5GXD6
• F5H6J7
• O75963
• Q5TGK0
• Q5TGK1
• Q5TGK2

Gene Name

• GPR161

Ensembl ID

• ENST00000367835
• ENSP00000356809
• ENSG00000143147
• ENST00000367836
• ENSP00000356810
• ENST00000367838
• ENSP00000356812
• ENST00000537209
• ENSP00000441039
• ENST00000539777
• ENSP00000437576
• ENST00000546300
• ENSP00000444348

Symbol

• RE2

Knowledge Table

Most Knowledge About	Knowledge Value (0 to 1 scale)
virus perturbation	0.94
histone modification site profile	0.76
disease perturbation	0.68
biological process	0.65
transcription factor	0.59

Protein Classes

DTO Classes

Protein / G-protein Coupled Receptor / Class A Rhodopsin Like / G-protein Coupled Receptor 161

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: 612.66   (req: < 5)

Gene RIFs: 9   (req: <= 3)

Antibodies: 243   (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: 612.66   (req: >= 5)

Gene RIFs: 9   (req: > 3)

Antibodies: 243   (req: > 50)

- OR - satisfy the following criterion:

Gene Ontology Terms: 4

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