Cited by 1,011Inflammatory mediators and NSAID effectsReceptor Mechanisms and SignalingEicosanoids and Hypertension Pharmacology

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Prostanoid Receptors: Subtypes and Signaling

Breyer, Richard M, Bagdassarian, Carey K, Myers, Scott A, Breyer, Matthew D·2001·Annual Review of Pharmacology and Toxicology

DOI 10.1146/annurev.pharmtox.41.1.661

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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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Authors: Breyer, R. M., Bagdassarian, C. K., Myers, S. A., & Breyer, M. D.
Affiliations: United States Department of Veterans Affairs (US)
ORCID: Breyer, Richard M
Breyer, Matthew D
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
DOI: 10.1146/annurev.pharmtox.41.1.661
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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