Prostaglandin receptor

Source: Wikipedia, the free encyclopedia.

Prostaglandin receptors or prostanoid receptors represent a sub-class of cell surface membrane

PGH2.[1]
They are named based on the prostanoid to which they preferentially bind and respond, e.g. the receptor responsive to PGI2 at lower concentrations than any other prostanoid is named the Prostacyclin receptor (IP). One exception to this rule is the receptor for thromboxane A2 (TP) which binds and responds to PGH2 and TXA2 equally well.

All of the prostanoid receptors are G protein-coupled receptors belonging to the Subfamily A14 of the rhodopsin-like receptor family except for the Prostaglandin DP2 receptor which is more closely related in amino acid sequence and functionality to chemotactic factor receptors such as the receptors for C5a and leukotriene B4.[2]

Prostanoid receptors bind and respond principally to metabolites of the straight chain

double bonds and are named series 2 prostanoids, i.e. PGD2, PGE2, PGF2α, PGI2, TXA2 and PGH2. However, the same enzymes that metabolize arachidonic acid to series 2 prostanoids similarly metabolize two other straight chain PUFAs: they metabolize gamma-Linolenic acid, which has one less double bond than arachidonic acid, to series 1 prostanoids (PGD1, PGE1, etc.), which have one less double bond than the series 2 prostanoids, and they metabolize eicosapentaenoic acid, which has one more double bond than arachidonic acid, to series 3 prostanoids (PGD3, PGE3, etc.), which have one more double bond than the series 2 prostanoids. In general, receptors for the series 2 prostanoids also bind with and respond to the series 1 and 3 prostanoids. Typically, prostanoid receptors show somewhat less affinity and responsiveness to the 1 and 3 series prostanoids.[3]

There are 9 established prostanoid receptors. The following table gives these receptors: a) full name; b) shortened names; c) activating prostanoids (presented in order of decreasing potencies);

cAMP response element-binding protein (CREB) which when activated phosphorylate and thereby influence the activity of key proteins that govern cell function.[2]

Full name shortened name activating prostanoids classification[5] G protein linkage[2] pathways[2]
Prostaglandin DP1 receptor
DP1
 PGD2>>PGE2>PGF2α>PGI2=TXA2[6] relaxant Gs alpha subunit activates AC, increases cAMP, raises Ca2+
Prostaglandin DP2 receptor
DP2
 PGD2>>PGF2α=PGE2>PGI2=TXA2[7] ? Gi alpha subunit inhibits AC to depress cAMP levels
Prostaglandin EP1 receptor
EP1
 PGE2>PGF2α=PGI2>PGD2=TXA2[8] contractile Gq alpha subunit stimulates PLC, IP3, PKC, ERK, p38 Mpk, and CREB
Prostaglandin EP2 receptor
EP2
 PGE2>PGF2α=PGI2>PGD2=TXA2[9] relaxant Gs alpha subunit stimulates AC, raises cAMP, stimulates
beta catenin
and Glycogen synthase kinase 3
Prostaglandin EP3 receptor
EP3
 PGE2>PGF2α,PGI2>PGD2=TXA2[10] inhibitory Gi & G12 subunit inhibits AC, decreases cAMP, stimulates PLC & IP3, raises Ca2+
Prostaglandin EP4 receptor
EP4
 PGE2>PGF2α=PGI2>PGD2=TXA2[11] relaxant Gs alpha subunit stimulates AC, PKA, PI3K, AKT, ERK, p38 Mpk, & CREB; raises cAMP
Prostaglandin F2α receptor
FP
 PGF2α>PGD2>PGE2>PGI2=TXA2[12] contractile Gq alpha subunit stimulates PLC, IP3, & PKC; raises Ca2+
Prostacyclin I2 receptor IP PGI2>>PGD2=PGE2=PGF2α>TXA2[13] relaxant Gs alpha subunit stimulates AC & PKA; raises cAMP
Thromboxane A2 receptor TP TXA=PGH2>>PGD2=PGE2=PGF2α=PGI2[14] contractile Gq alpha subunit stimulates PLC & IP3; raises Ca2+

There is indirect evidence for a second PGI2 receptor in BEAS-2B human airway epithelial cells but this finding has not been collaborated and the putative receptor has not been otherwise defined.[15]

See also

References

  1. PMID 12432942
    .
  2. ^
    S2CID 1513449
    .
  3. S2CID 7766467
    .
  4. ^ a b "Prostanoid receptors - G protein-coupled receptors - IUPHAR/BPS Guide to PHARMACOLOGY". www.guidetopharmacology.org.
  5. ^
    S2CID 207058745
    .
  6. ^ "DP1 receptor - Prostanoid receptors - IUPHAR/BPS Guide to PHARMACOLOGY". www.guidetopharmacology.org.
  7. ^ "DP2 receptor - Prostanoid receptors - IUPHAR/BPS Guide to PHARMACOLOGY". www.guidetopharmacology.org.
  8. ^ "EP1 receptor - Prostanoid receptors - IUPHAR/BPS Guide to PHARMACOLOGY". www.guidetopharmacology.org.
  9. ^ "EP2 receptor - Prostanoid receptors - IUPHAR/BPS Guide to PHARMACOLOGY". www.guidetopharmacology.org.
  10. ^ "EP3 receptor - Prostanoid receptors - IUPHAR/BPS Guide to PHARMACOLOGY". www.guidetopharmacology.org.
  11. ^ "EP4 receptor - Prostanoid receptors - IUPHAR/BPS Guide to PHARMACOLOGY". www.guidetopharmacology.org.
  12. ^ "FP receptor - Prostanoid receptors - IUPHAR/BPS Guide to PHARMACOLOGY". www.guidetopharmacology.org.
  13. ^ "IP receptor - Prostanoid receptors - IUPHAR/BPS Guide to PHARMACOLOGY". www.guidetopharmacology.org.
  14. ^ "TP receptor - Prostanoid receptors - IUPHAR/BPS Guide to PHARMACOLOGY". www.guidetopharmacology.org.
  15. S2CID 11882621
    .

External links
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