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Prostanoid Receptors: Subtypes and Signaling
Abstract
Cyclooxygenases metabolize arachidonate to five primary prostanoids: PGE 2, PGF 2α, PGI 2, TxA 2, and PGD 2. These autacrine lipid mediators interact with specific members of a family of distinct G-protein-coupled prostanoid receptors, designated EP, FP, IP, TP, and DP, respectively. Each of these receptors has been cloned, expressed, and characterized. This family of eight prostanoid receptor complementary DNAs encodes seven transmembrane proteins which are typical of G-protein-coupled receptors and these receptors are distinguished by their ligand-binding profiles and the signal transduction pathways activated on ligand binding. Ligand-binding selectivity of these receptors is determined by both the transmembrane sequences and amino acid residues in the putative extracellular-loop regions. The selectivity of interaction between the receptors and G proteins appears to be mediated at least in part by the C-terminal tail region. Each of the EP 1, EP 3, FP, and TP receptors has alternative splice variants described that alter the coding sequence in the C-terminal intracellular tail region. The C-terminal variants modulate signal transduction, phosphorylation, and desensitization of these receptors, as well as altering agonist-independent constitutive activity.
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From Platelets induce increased estrogen production through NF-κB and TGF-β1 signaling pathways in endometriotic stromal cells (2020) · cites this paper as [14]
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Metadata
- Authors
- Breyer, R. M., Bagdassarian, C. K., Myers, S. A., & Breyer, M. D.
- Affiliations
- United States Department of Veterans Affairs (US)
- Venue
- Annual Review of Pharmacology and Toxicology
- Publisher
- Annual Reviews
- Published
- 2001-04
- Volume
- 41
- Issue
- 1
- Pages
- 661-690
- ISSN
- 0362-1642 (ISSN-L)
- 1545-4304
- OpenAlex
- W2129746956
- Cited by
- 1,011
- References
- 152
- Citations by year
- 2026: 7 · 2025: 17 · 2024: 11 · 2023: 22 · 2022: 17 · 2021: 27 · 2020: 37 · 2019: 22 · 2018: 24 · 2017: 32 · 2016: 38 · 2015: 43 · 2014: 50 · 2013: 40 · 2012: 51
- FWCI
- 5.37
- Type
- journal article
- Language
- en
- Open access
- closed
- Locations
- The Annual Review of Pharmacology and Toxicology (publishedVersion)
- PubMed (publishedVersion)
- Funders
- National Institute of General Medical Sciences (GM 15431)
- National Institute of Diabetes and Digestive and Kidney Diseases (DK37097, DK46205, R01DK037097, R01DK046205)
- Topics
- Health Sciences › Medicine › Pharmacology (medical) › Inflammatory mediators and NSAID effects
- Life Sciences › Biochemistry, Genetics and Molecular Biology › Molecular Biology › Receptor Mechanisms and Signaling
- Life Sciences › Biochemistry, Genetics and Molecular Biology › Biochemistry › Eicosanoids and Hypertension Pharmacology
- Keywords
- prostanoid receptors, G protein-coupled receptors, prostaglandins, cyclooxygenase, arachidonic acid metabolism, prostaglandin E2, prostaglandin F2alpha, prostacyclin, thromboxane A2, prostaglandin D2, receptor subtypes, ligand selectivity, splice variants, receptor desensitization, receptor phosphorylation, constitutive receptor activity, signal transduction
- MeSH terms
- Amino Acid Sequence, Animals, Humans, Molecular Sequence Data, Prostaglandins, Receptors, Prostaglandin, Signal Transduction
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