Prostaglandin DP2 receptor

Prostaglandin D2 receptor 2 (DP2) is a human protein encoded by the PTGDR2 gene. DP2 has also been designated as CD294 (cluster of differentiation 294).

Function

G protein-coupled receptors (GPCRs), such as DP2, are integral membrane proteins containing 7 putative transmembrane domains (TMs). These proteins mediate signals to the interior of the cell via activation of heterotrimeric G proteins that in turn activate various effector proteins, ultimately resulting in a physiologic response.[supplied by OMIM]

DP2 has recently been found when activated by elevated level of prostaglandin D2 (PGD2), it could inhibit hair growth. This suggests the DP2 pathway as a potential target for bald treatment. A particularly promising compound for blocking the DP2 pathway is a compound known as TM30089, which exhibits a "functional insurmountability" of PGD2 expression.

Ligands

Agonists

  • Indometacin - non-selective
  • Prostaglandin D2 - non-selective
  • Antagonists

  • ADC-3680 - selective
  • AZD-1981 - selective
  • Prostaglandin DP1 receptor

    Prostaglandin D2 receptor 1 (DP1) is a G protein-coupled receptor, encoded by the PTGDR1 gene, for prostaglandin D2 (PGD2).

    Mechanism

    DP1 is a G protein-coupled receptor (GPCR). Its activity is mainly mediated by G-S proteins that stimulate adenylate cyclase resulting in an elevation of intracellular cAMP and Ca2+.

    Function

    Knockout studies in mice suggest that the ligand of this receptor, prostaglandin D2, functions as a mast cell-derived mediator to trigger asthmatic responses. It also causes vasodilation

    Ligands

  • Prostaglandin D2 - non-selective
  • Treprostinil - non-selective
  • Asapiprant (S-555739) - selective
  • Laropiprant - selective
  • Vidupiprant - dual DP1 and DP2 antagonist
  • See also

  • Prostaglandin DP2 receptor
  • Eicosanoid receptor
  • References

    External links

  • "Prostanoid Receptors: DP1". IUPHAR Database of Receptors and Ion Channels. International Union of Basic and Clinical Pharmacology. 
  • Further reading

    This article incorporates text from the United States National Library of Medicine, which is in the public domain.

    Prostaglandin D2 receptor

    The prostaglandin D2 (PGD2) receptors are G protein-coupled receptors that bind and are activated by prostaglandin D2. They include the following proteins:

  • Prostaglandin D2 receptor 1 (DP1) - PTGDR1
  • Prostaglandin D2 receptor 2 (DP2) - PTGDR2
  • See also

  • Eicosanoid receptor
  • Prostaglandin E2 receptor
  • References

    External links

  • Prostaglandin D2 Receptors at the US National Library of Medicine Medical Subject Headings (MeSH)


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