Target intelligence / Profile preview

Sphingosine-1-phosphate receptor 1; Sphingosine-1-phosphate receptor 5 (S1PR1; S1PR5)

Target
S1PR1; S1PR5
Molecular classification
G protein-coupled receptor, Receptor, Seven-transmembrane domain receptor
01

Overview

Sphingosine-1-phosphate receptor 1 (S1PR1) and sphingosine-1-phosphate receptor 5 (S1PR5) are members of the S1P receptor family (S1PR1–5), which are G protein-coupled, seven-transmembrane domain receptors. Both receptors bind the sphingolipid S1P, mediating a variety of physiological effects. S1PR1 is widely expressed, especially on endothelial and immune cells, and is vital for lymphocyte circulation, endothelial barrier regulation, and vascular maturation. S1PR5 is expressed primarily in the central nervous system (oligodendrocytes, white matter) and spleen, but also on certain immune cells such as natural killer cells and patrolling monocytes, where it regulates cell trafficking. Both receptors are established therapeutic targets, particularly in immunological and neurodegenerative disorders, with several approved drugs (notably S1P receptor modulators) exerting immunosuppressive effects by modulating receptor function

Other names
S1PR1Endothelial differentiation gene 1 (EDG1)S1PR5Endothelial differentiation gene 8 (EDG8)
02

Mechanism of action

Functional antagonism (induced receptor internalization and downregulation) Blockade of lymphocyte egress from lymph nodes (immunomodulation/immune cell sequestration) Modulation of vascular permeability and endothelial barrier integrity Regulation of cell migration in the CNS and peripheral tissues

03

Biological functions

Signal transductionImmune cell traffickingVascular maturation and barrier regulationCell migrationNervous system cell migration and egressRegulation of endothelial cell function
04

Disease associations

Autoimmune disease (notably multiple sclerosis)InflammationCancerNeurodegenerative diseaseCardiovascular disease
05

Safety considerations

Bradycardia and conduction disturbances (AV block, especially on first-dose)Macular edemaRisk of infection (due to immunosuppression)Liver function abnormalitiesRare sudden cardiac deathHypertension
06

Interacting drugs

Fingolimod (non-selective, S1PR1/3/4/5)

3 more in the full profile.

07

Biomarkers

Lymphocyte count (for monitoring efficacy and immune status in treated patients)Cardiac function (heart rate and conduction assessment before and during therapy)

Beyond the preview

Go deeper on Sphingosine-1-phosphate receptor 1; Sphingosine-1-phosphate receptor 5 (S1PR1; S1PR5).

Explore the evidence, development activity, and competitive landscape with Gosset’s full data platform.

Drug pipeline

Full profile access

Explore the programs pursuing this target and their development progress.

  • Drug candidates
  • Developers
  • Development stage

Clinical trials

Full profile access

Follow the clinical studies evaluating therapies directed at this target.

  • Trial design
  • Status
  • Readouts

Competitive landscape

Full profile access

Compare approaches across drug candidates, modalities, and indications.

  • Programs
  • Modalities
  • Indications

Literature & evidence

Full profile access

Investigate the research and source evidence behind target biology and development.

  • Publications
  • Sources
  • Analysis

Patents

Full profile access

Explore patent activity around therapies and technologies addressing this target.

  • Patents
  • Assignees
  • Technologies

Research & analysis

Full profile access

Connect target biology, drug development, and emerging evidence in your research.

  • Biology
  • Development news
  • Analysis

Bring the full picture into focus.

See how Gosset can support your research on Sphingosine-1-phosphate receptor 1; Sphingosine-1-phosphate receptor 5 (S1PR1; S1PR5).

Explore the full profile

Gosset Free

Get started with Gosset.

Enter your work email and we’ll be in touch with next steps.

Work email preferred.

Book a call