Sphingosine-1-phosphate receptor

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Sphingosine-1-phosphate receptor
Sphingosine-1-phosphate receptor rendering
Identifiers
Symbol?

The sphingosine-1-phosphate receptors are a class of

G protein-coupled receptors that are targets of the lipid signalling molecule Sphingosine-1-phosphate (S1P). They are divided into five subtypes: S1PR1, S1PR2, S1PR3, S1PR4 and S1PR5
.

Discovery

In 1990, S1PR1 was the first member of the S1P receptor family to be cloned from

cDNA library.[4][5]

Function

The sphingosine-1-phosphate receptors regulate fundamental biological processes such as cell proliferation,

Subtypes

Sphingosine-1-phosphate (S1P) receptors are divided into five subtypes: S1PR1, S1PR2, S1PR3, S1PR4 and S1PR5.

They are expressed in a wide variety of tissues, with each subtype exhibiting a different cell specificity, although they are found at their highest density on

hematopoietic tissues whereas S1PR5 primarily located in the white matter of the central nervous system (CNS) and spleen
.

G protein interactions and selective ligands

The sphingosine-1-phosphate (S1P) is the endogenous agonist for the five subtypes.

Receptor G protein-coupled receptor superfamily Agonists Antagonists
S1PR1
  • Gi/Go family
  • W146 (CAS# 909725-62-8)[15]
  • VPC 23019 (CAS# 449173-19-7)[16]
S1PR2
  • Gs family
  • Gq/G11 family
  • G12/G13 family
  • S1P
  • JTE 013 (547756-93-4)[17]
  • AB1 (1463912-49-3)[18]
S1PR3
  • Gi/Go family
  • Gq/G11 family
  • G12/G13 family
  • S1P
  • Fingolimod (162359-55-9)[12]
  • VPC 23019 (CAS# 449173-19-7)[16]
S1PR4
  • Gi/Go family
  • G12/G13 family
  • S1P
  • Fingolimod (162359-55-9)[12]
  • CYM 50260 (CAS# 1355026-60-6)[19]
  • CYM 50308 (CAS# 1345858-76-5)[20]
  • JTE 013 (547756-93-4)[21]
S1PR5
  • Gi/Go family
  • G12/G13 family
  • S1P
  • Fingolimod (162359-55-9)[12]
  • Ozanimod (1306760-87-1)[13]

References