GPR161
GPR161 (G protein-coupled receptor 161) is a gene. In the public catalogues the evidence so far is association rather than a proven role. Tied to Medulloblastoma.
Overview
G protein-coupled receptor that acts as a key inhibitor of the smoothened signalling pathway in primary cilia. Inhibits the smoothened signalling pathway in absence of hedgehog (DHH, IHH or SHH) by promoting formation of the transcription repressor form of GLI2 and GLI3 transcription factors. GPR161 activation triggers signalling via guanine nucleotide-binding protein G(s)/GNAS, mediating activation of adenylate cyclase activity and production of cAMP.
- Target · the protein and the cell it sits on
- Drug · antibody, small molecule, cell or radioligand
- Effect · signal, damage or kill
In plain words · GPR161 (G protein-coupled receptor 161) is a gene. In the public catalogues the evidence so far is association rather than a proven role. Tied to Medulloblastoma.
- 1 · What it is
GPR161 (G protein-coupled receptor 161) is a gene. In the public catalogues the evidence so far is association rather than a proven role. Tied to Medulloblastoma.
- 2 · What goes wrong in cancer
G protein-coupled receptor that acts as a key inhibitor of the smoothened signalling pathway in primary cilia.
- 3 · How drugs use it
No product in this corpus aims at GPR161 yet. Drugs bind the molecule precisely: to switch it off, flag the cell for the immune system, or deliver a payload.
External identifiers
Sources: HGNC HGNC:23694 (approved symbol, name, aliases, locus and cross-references (hgnc_complete_set.txt)); UniProt Q8N6U8 (protein name, function text, keywords and locations (REST API)); Open Targets ENSG00000143147 (per-cancer scores at or above 0.5: medulloblastoma 0.64 (GraphQL API, CC0))
Biology
G protein-coupled receptor that acts as a key inhibitor of the smoothened signalling pathway in primary cilia. Inhibits the smoothened signalling pathway in absence of hedgehog (DHH, IHH or SHH) by promoting formation of the transcription repressor form of GLI2 and GLI3 transcription factors. GPR161 activation triggers signalling via guanine nucleotide-binding protein G(s)/GNAS, mediating activation of adenylate cyclase activity and production of cAMP. Increased cAMP levels activate PKA, promoting PKA-dependent processing of GLI2 and GLI3 transcription factors, leading to formation of transcription repressor GLI2R and GLI3R, which repress expression of target genes. GPR161 also activates PKA by acting as a PKA-anchoring protein, which directly associates with type I PKA regulatory subunits (PRKAR1A and/or PRKAR1B), recruiting PKA followed by PKA-dependent processing of GLI2 and GLI3 transcription factors. In presence of hedgehog, GPR161 is removed from primary cilia by smoothened (SMO), preventing its activity and allowing activation of the smoothened signalling. Location: Cell projection, cilium membrane; Cell membrane (UniProt). Locus 1q24.2 (HGNC).
- Medulloblastoma: Open Targets association 0.64 with medulloblastoma (MONDO_0007959)
Notes
top- Written by scripts/fetch-cancer-genes.ts from CIViC, Open Targets, IntOGen, HGNC and UniProt; the function text is UniProt's, condensed and in UK spelling. Roles: none stated by the sources. Evidence tier "association-only" is the strongest of those signals.
- Prevalence not recorded: none of the sources gives a positivity rate.
Latest papers
topQuery for this target: (TITLE:"GPR161" OR ABSTRACT:"GPR161" OR TITLE:"G protein-coupled receptor 161" OR ABSTRACT:"G protein-coupled receptor 161" OR TITLE:"RE2" OR ABSTRACT:"RE2") AND (cancer OR tumor OR tumour OR oncology OR carcinoma OR lymphoma OR leukemia OR leukaemia OR myeloma OR sarcoma OR melanoma OR glioma). Results are unfiltered search hits about GPR161, not a curated reading list.
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