Back to discover

Protein / target

Sigma non-opioid intracellular receptor 1

Encoded bySIGMAR1Q99720Homo sapiensSwiss-Prot
Clinically validated
Therapeutic maturity
9
Approved medicines
Open Targets target-level
Small-molecule tractable
Druggability
Approved Drug
1
Research papers

Protein at a glance

Biological role

G protein-coupled opioid receptor

Therapeutic position

Established drug target

Small molecules

Research activity

Emerging research

1 papers · latest 2024

Derived from structured UniProt, Open Targets and literature data on this page.

Protein profile

UniProt 2026_02

Canonical identity and biological annotation from UniProt.

Function overview

Functions in lipid transport from the endoplasmic reticulum and is involved in a wide array of cellular functions probably through regulation of the biogenesis of lipid microdomains at the plasma membrane.

View complete UniProt function annotation

Functions in lipid transport from the endoplasmic reticulum and is involved in a wide array of cellular functions probably through regulation of the biogenesis of lipid microdomains at the plasma membrane. Involved in the regulation of different receptors it plays a role in BDNF signaling and EGF signaling. Also regulates ion channels like the potassium channel and could modulate neurotransmitter release. Plays a role in calcium signaling through modulation together with ANK2 of the ITP3R-dependent calcium efflux at the endoplasmic reticulum. Plays a role in several other cell functions including proliferation, survival and death. Originally identified for its ability to bind various psychoactive drugs it is involved in learning processes, memory and mood alteration (PubMed:16472803, PubMed:9341151). Necessary for proper mitochondrial axonal transport in motor neurons, in particular the retrograde movement of mitochondria. Plays a role in protecting cells against oxidative stress-induced cell death via its interaction with RNF112 (By similarity)

Subcellular location

Nucleus inner membraneNucleus outer membraneNucleus envelopeCytoplasmic vesicleEndoplasmic reticulum membraneMembraneLipid dropletCell junctionCell membraneCell projection, growth conePostsynaptic density membrane
Domains and Gene Ontology detail (31)

Gene Ontology

  • Canchoring junction
  • Ccytoplasmic vesicle
  • Ccytosol
  • Cdendrite
  • Cendoplasmic reticulum
  • Cendoplasmic reticulum membrane
  • Cglutamatergic synapse
  • Cgrowth cone
  • Clipid droplet
  • Cmembrane
  • Cneuronal cell body
  • Cnuclear envelope

223 aa · 25 kDa · 5 isoforms

Biological roles

What this protein does, drawn together from its UniProt function, Gene Ontology terms and Reactome pathways.

Synaptic signallingUniProt · GOLipid & lipoprotein metabolismUniProt · GOApoptosis & cell deathGO
View supporting evidence

Synaptic signalling

  • ·Postsynaptic density membrane
  • ·glutamatergic synapse
  • ·postsynaptic density
  • ·postsynaptic density membrane

Lipid & lipoprotein metabolism

  • ·Functions in lipid transport from the endoplasmic reticulum and is involved in a wide ar…
  • ·lipid transport

Apoptosis & cell death

  • ·negative regulation of neuron apoptotic process
  • ·regulation of neuron apoptotic process

Concepts derived from UniProt GO Reactome — each badge above shows which sources supported that role.

Translational evidence

Open Targets 26

Why this target matters therapeutically, strongest evidence first. Disease associations are gene-level (via the gene that encodes this protein) and open into the full confidence synthesis; the development universe, tractability and safety annotations are target-level, from Open Targets.

Drug development

9 compounds recorded · 9 approved

Open Targets' development universe — every compound recorded against the target at any stage, not all approved medicines.

View all recorded compounds (9)
DEXTROMETHORPHANApproval
FENFLURAMINEApproval
DEXTROMETHORPHAN HYDROBROMIDEApproval
PENTAZOCINE HYDROCHLORIDEApproval
CARBETAPENTANE CITRATEApproval
DEXTROMETHORPHAN POLISTIREXApproval
PENTAZOCINEApproval
FENFLURAMINE HYDROCHLORIDEApproval
CARBETAPENTANEApproval

Open Targets known-drugs universe. Drug name and highest clinical stage only — the disease relationship is NOT read from this slice (it carries trial-context noise); approved indications come from the canonical graph above.

Tractability

Small moleculesStrong

Approved Drug and Structure with Ligand support this modality.

AntibodiesEmerging

Feasibility evidence (uniprot loc high conf and uniprot sigp or tmhmm) — no clinical-stage drug of this modality recorded.

Protein degradersEmerging

Feasibility evidence (database ubiquitination and half-life data) — no clinical-stage drug of this modality recorded.

View underlying tractability evidence (10)
SM · Approved DrugSM · Structure with LigandSM · High-Quality LigandSM · Druggable FamilyAB · UniProt loc high confAB · UniProt SigP or TMHMMAB · GO CC med confPR · Database UbiquitinationPR · Half-life DataPR · Small Molecule Binder

Raw Open Targets tractability assessment buckets, by modality.

Safety-related annotations

decreased painLynch et al. (2017)hallucinationsLynch et al. (2017)decreased anxietyLynch et al. (2017)decreased convulsionsLynch et al. (2017)increased memoryLynch et al. (2017)drug abuse/dependenceLynch et al. (2017)

Terms indexed against this target in Open Targets' safety data, with their datasource. These are annotations, not causal claims: the direction of effect (whether activation or inhibition is implicated), species and evidence strength are not captured here, so an entry does not mean that modulating this target is known to cause that condition.

Research activity

1 papers · to 2024

Papers linked directly to this protein. This is the protein's own literature — descriptor-derived papers are kept separate below.

Most cited

Recent

Europe PMC papers linked directly to this protein.