Prostaglandin DP1 receptor
Appearance
Prostaglandin D2 receptor 1 (DP1) is a G protein-coupled receptor, encoded by the PTGDR1 gene, for prostaglandin D2 (PGD2).[5] Template:PBB Summary
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.[5] It also causes vasodilation.
Ligands
- Agonists
- Prostaglandin D2 - non-selective
- Treprostinil - non-selective
- Antagonists [6]
- Asapiprant (S-555739) - selective
- Laropiprant - selective
- Vidupiprant - dual DP1 and DP2 antagonist
See also
References
- ^ a b c GRCh38: Ensembl release 89: ENSG00000168229 – Ensembl, May 2017
- ^ a b c GRCm38: Ensembl release 89: ENSMUSG00000071489 – Ensembl, May 2017
- ^ "Human PubMed Reference:". National Center for Biotechnology Information, U.S. National Library of Medicine.
- ^ "Mouse PubMed Reference:". National Center for Biotechnology Information, U.S. National Library of Medicine.
- ^ a b "Entrez Gene: PTGDR prostaglandin D2 receptor (DP)".
- ^ Norman P (Jan 2014). "Update on the status of DP2 receptor antagonists; from proof of concept through clinical failures to promising new drugs". Expert Opin Investig Drugs. 23 (1): 55–66. doi:10.1517/13543784.2013.839658. PMID 24073896.
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.