Prostanoid receptors: subtypes and signaling

RM Breyer, CK Bagdassarian, SA Myers… - Annual review of …, 2001 - annualreviews.org
RM Breyer, CK Bagdassarian, SA Myers, MD Breyer
Annual review of pharmacology and toxicology, 2001annualreviews.org
Cyclooxygenases metabolize arachidonate to five primary prostanoids: PGE2, PGF2α, PGI2,
TxA2, and PGD2. 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 …
Cyclooxygenases metabolize arachidonate to five primary prostanoids: PGE2, PGF, PGI2, TxA2, and PGD2. 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 EP1, EP3, 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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