Protein / target
Sphingosine 1-phosphate receptor 1
Protein at a glance
Biological role
Sphingosine-1-phosphate receptor activity
Primary system
Cardiovascular system
Strongest disease association
hypothyroidism
Therapeutic maturity
Clinically validated target
Druggability
Small molecule
Clinical development
10 approved · 4 in clinical development
Derived from structured UniProt, Open Targets and literature data on this page.
Protein profile
Canonical identity and biological annotation from UniProt.
Function
G protein-coupled receptor for the bioactive lysosphingolipid sphingosine 1-phosphate (S1P) that seems to be coupled to the G(i) subclass of heteromeric G proteins. Signaling leads to the activation of RAC1, SRC, PTK2/FAK1 and MAP kinases. Plays an important role in cell migration, probably via its role in the reorganization of the actin cytoskeleton and the formation of lamellipodia in response to stimuli that increase the activity of the sphingosine kinase SPHK1. Required for normal chemotaxis toward sphingosine 1-phosphate. Required for normal embryonic heart development and normal cardiac morphogenesis. Plays an important role in the regulation of sprouting angiogenesis and vascular maturation. Inhibits sprouting angiogenesis to prevent excessive sprouting during blood vessel development. Required for normal egress of mature T-cells from the thymus into the blood stream and into peripheral lymphoid organs. Plays a role in the migration of osteoclast precursor cells, the regulation of bone mineralization and bone homeostasis (By similarity). Plays a role in responses to oxidized 1-palmitoyl-2-arachidonoyl-sn-glycero-3-phosphocholine by pulmonary endothelial cells and in the protection against ventilator-induced lung injury
Subcellular location
Domains and Gene Ontology detail (35)Hide
Gene Ontology
- Ccytoplasm
- Cendosome
- Cexternal side of plasma membrane
- Cmembrane raft
- Cplasma membrane
- Cpresynapse
- FG protein-coupled receptor activity
- FG protein-coupled receptor binding
- Fsphingolipid binding
- Fsphingosine-1-phosphate receptor activity
- Pactin cytoskeleton organization
- Padenylate cyclase-activating G protein-coupled receptor signaling pathway
Biological roles
What this protein does, drawn together from its UniProt function, Gene Ontology terms and Reactome pathways.
View supporting evidenceHide supporting evidence
G protein-coupled signalling
- ·G protein-coupled receptor for the bioactive lysosphingolipid sphingosine 1-phosphate (S…
- ·G protein-coupled receptor activity
- ·G protein-coupled receptor binding
- ·adenylate cyclase-activating G protein-coupled receptor signaling pathway
Immune signalling
- ·T cell migration
- ·Interleukin-4 and Interleukin-13 signaling
Synaptic signalling
- ·presynapse
Cell adhesion
- ·cell adhesion
Transcriptional regulation
- ·positive regulation of transcription by RNA polymerase II
View underlying pathways (3)Hide underlying pathways
Concepts derived from UniProt GO Reactome — each badge above shows which sources supported that role.
Interaction neighbourhood
Proteins with the strongest functional or physical association. Node size and line weight reflect STRING confidence; hover or select a partner to inspect one association.
Functional and physical associations from STRING v12.0. Only associations with this protein are drawn — partner-to-partner links are not part of this evidence.
Drugs targeting this protein
Whether each drug engages this protein directly or through a complex, and how many other targets are recorded for it. Direct binders with few recorded targets are listed first.
Sphingosine 1-phosphate receptor agonist
Appears in clinical studies involving multiple sclerosis, relapsing-remitting multiple sclerosis, kidney transplant
ChEMBL mechanism, action type and target identity. Open Targets clinical status and indications.
Translational evidence
Why this target matters therapeutically — disease associations, drugs in development, tractability and safety, from Open Targets.
Strongest genetic associations
Human genetic evidence — the most direct causal link between this target and a disease.
Highest-confidence therapeutic associations
Diseases where a drug acting on this target has already reached clinical development.
Highest overall evidence
Remaining associations by Open Targets' aggregated evidence score.
Show all associationsHide all associations
Open Targets ranks 651 associations for this target and we store the top 10 by aggregated score. The long tail is largely literature co-mention and RNA-expression evidence, not evidence that this target drives those diseases.
Known drugs · 14 total
systemic lupus erythematosus · lupus nephritis
Crohn disease · multiple sclerosis · psoriasis
ulcerative colitis · multiple sclerosis · systemic lupus erythematosus
multiple sclerosis · relapsing-remitting multiple sclerosis · chronic progressive multiple sclerosis
ulcerative colitis · Crohn disease · atopic eczema
multiple sclerosis · relapsing-remitting multiple sclerosis · psoriasis vulgaris
ulcerative colitis
multiple sclerosis · ulcerative colitis · relapsing-remitting multiple sclerosis
multiple sclerosis · non-small cell lung carcinoma · ulcerative colitis
primary progressive multiple sclerosis · multiple sclerosis · relapsing-remitting multiple sclerosis
Tractability
Clinical trials
Trials of drugs that target this protein — reached indirectly through those drugs, so a trial listed here studies the drug, not the protein.
ClinicalTrials.gov via the drug-target graph.
Forefront confidence
Our own weighting of the evidence behind each disease association. Human genetics and clinical evidence count for most; literature co-mention counts for little, because two entities sharing an abstract is not evidence that one drives the other.
The evidence agreement range shows how closely the independent evidence families agree — it is not a statistical confidence interval, and nothing here is fitted to outcome data. Derived from Open Targets evidence types under Forefront weighting; the underlying per-type scores are shown above so the calculation can be checked.
What's happening now
Recent activity around this target, drawn from one canonical event stream. Every item is reached through a drug that targets this protein, so each event is news about that drug rather than about the protein directly.
- New publicationGlial Sphingosine-Mediated Epigenetic Regulation Stabilizes Synaptic Function in <i>Drosophila</i> Models of Alzheimer's Disease.
- Regulatory approval
Approval: Fingolimod Accord (EMA)
- Regulatory approval
Approval: Gilenya (EMA)
Objective event titles are shown unmodified; the event kind and significance line are derived from structured fields. Forefront AttentionEvent stream aggregating Europe PMC Regulatory filings ClinicalTrials.gov.