Target Atlas

Computational Target Profile

GPR176

IDG Tbio

A Gz-coupled orphan receptor tied to the circadian clock, characterised without an experimental structure.

An orphan that helps set the pace of the circadian clock — Gz-coupled, repressing cAMP with agonist-independent basal activity, and lately tied to cancer progression too. No solved structure, no confirmed ligand — resolved into a topology, a residue-level binding-pocket hypothesis, and a validation plan.

UniProt Q14439 ·AFDB AF-Q14439-F1 ·515 aa·Class A (rhodopsin-like) orphan GPCR·PDB: none
At a Glance
Fold
Seven transmembrane helices; multi-pass plasma-membrane receptor; non-enzyme.
Binding Pocket
Predicted binding pocket (AstraBIND confidence 0.767, high). A residue-level cavity in the class A helical bundle (TM6, TM7) — a starting point for docking and mutagenesis; unclassified, with no validated ligand.
Structural Anchors
N-glycosylation on the extracellular N-terminus — predicted sequons at N4, N11, N17 and N27, experimentally confirmed (Wang 2020).
Flexible Regions
Elevated predicted disorder — disordered N-terminus (1–31) and an unusually long cytoplasmic C-tail (346–511) — the natural truncation boundaries for construct design.
Clean Signal
No amyloidogenic segments predicted.
Prediction Confidence
7 TM Helices
1.00
Multi-Pass Membrane
0.99
Receptor Class
1.00
G-Protein-Coupled Receptor Activity (GO)
0.85
Binding Pocket
0.77

Model-reported confidence for the headline calls (amber = the load-bearing prediction the rest of the profile builds on). These are model-estimated probabilities that rank and gate each call — not calibrated rates of experimental success.

The Gap

Why This Target Is Still Dark

Most tractable receptor families have been structurally explored. GPR176 remains dark: an IDG Tbio class A GPCR with no experimental structure in the PDB and no confirmed ligand. Its defining feature is constitutive: it couples to the G(z) subclass and, without any agonist, holds cAMP production repressed — a basal tone reported to help set the pace of circadian behaviour in the brain's master clock. More recent work links it to cancer progression, giving a second, independent reason to characterise it.

That combination — genuine interest, near-zero structural information — is exactly where prediction earns its keep: everything below is computed from the canonical 515-residue sequence with Orbion's Astra suite, with no experimental GPR176 structure or validated ligand used as input. For a genuine orphan, there is nothing to look up.

Architecture & Topology

How the Sequence Is Organised

extracellularintracellularTM1TM2TM3TM4TM5TM6TM7NC
Pocket-Lining HelixTransmembrane Helix Disordered Loop
Predicted Membrane Topology · Pocket-Lining Helices in Amber · Disordered Loops Dashed · N/C Termini In Situ
ElementResiduesNote
Transmembrane Helices7 predictedBoundaries: 43–63; 83–103; 119–139; 161–181; 208–228; 268–288; 300–320.
Per-Residue Disorder
N-TermC-Tail00.511200400515
Disordered Regions Shaded in Amber · Dashed Line = 0.5 Call Threshold · the Natural Truncation Boundaries for Construct Design

The Predicted Pocket

A Predicted Binding Pocket

For this genuine orphan, AstraBIND has no ligand-bound relative to retrieve from — so these residues are a structure-based cavity prediction, not a retrieval-grounded pocket, and the score reflects cavity geometry rather than a known binding site. Treat them as an exploratory starting point for mutagenesis only; the topology, disorder and modification maps above are the higher-confidence outputs for this target. No validated ligand; not a proven druggable site.

Site: Class A helical bundle (extracellular-facing cavity)

Pocket-Lining Residues
TM6275, 279, 282
TM7304–310, 312, 316

Post-Translational & Structural Features

Specific, Testable Residues

  • N-glycosylation at position 4, 11, 17, 27 — a cluster on the extracellular N-terminus whose N-linked glycosylation has been functionally characterised for GPR176 (UniProt).
  • No amyloidogenic segments predicted. A clean aggregation profile across the sequence — one fewer liability for construct design.

Recommended Experimental Follow-Up

An Orphan Sequence, Turned Into a Ranked Plan

Each prediction is paired with the experiment that would test it and the readout to watch for.

PredictionExperimentReadout
Binding-Pocket Residues (TM6, TM7)Alanine scan + docking / fragment screen at the predicted pocketBinding or SAR at the predicted site
N-Glycosylation Cluster (N4, N11, N17, N27)N→Q mutagenesis of the N-terminal sitesTrafficking / surface-expression shift
Disordered N-Term (1–31) and Long C-Tail (346–511)Terminal truncation or fusion-partner insertionExpression / thermostability for structural work
Constitutive G(z) SignallingcAMP assay for agonist-independent basal activityConfirm G(z) coupling and basal cAMP repression

Scope & Limitations

What This Is — and Isn't

  • Prediction, not experiment. These are computational hypotheses to prioritise experiments — not a structure or an assay. Nothing here is wet-lab validated.
  • The pocket is predicted; the ligand is not named. AstraBIND is retrieval-based and here returns an unclassified cavity — a residue-level hypothesis, not a proven druggable site or a validated binder.
  • Biology from model systems, and maybe no ligand to find. GPR176's circadian role rests on mouse SCN studies and its cancer link on recent tumour work; because it signals constitutively through G(z) with no known agonist, there may be no classical orthosteric ligand at all. Treat both the pocket and the therapeutic case as hypotheses.

All predictions were generated with Orbion's Astra suite from the canonical GPR176 sequence (UniProt Q14439), using AlphaFold-derived structural features. Reported values are model outputs; model internals are out of scope.

References

  1. [1]UniProt Consortium. UniProtKB entry Q14439 (GPR176, human). uniprot.org.
  2. [2]Pharos (Illuminating the Druggable Genome). GPR176 target record — Tbio. pharos.nih.gov.
  3. [3]Doi M et al. Gpr176 is a Gz-linked orphan G-protein-coupled receptor that sets the pace of circadian behaviour. (2016). https://doi.org/10.1038/ncomms10583
  4. [4]Tang J et al. GPR176 Promotes Cancer Progression by Interacting with G Protein GNAS to Restrain Cell Mitophagy in Colorectal Cancer. (2023). https://doi.org/10.1002/advs.202205627
  5. [5]Wang T et al. Identification and functional characterisation of N-linked glycosylation of the orphan G protein-coupled receptor Gpr176. (2020). https://doi.org/10.1038/s41598-020-61370-y

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