Matches in SemOpenAlex for { <https://semopenalex.org/work/W3148296711> ?p ?o ?g. }
Showing items 1 to 66 of
66
with 100 items per page.
- W3148296711 endingPage "479" @default.
- W3148296711 startingPage "473" @default.
- W3148296711 abstract "Prostanoids [prostaglandins (PGs) and thromboxanes (TXs)] are a series of bioactive lipid metabolites that function in an autacoid manner via activation of cognate G protein-coupled receptors (GPCRs). The nine subtypes of prostanoid receptors (DP1, DP2, EP1, EP2, EP3, EP4, FP, IP, TP) are involved in a wide range of functions, including inflammation, immune response, reproduction, and homeostasis of the intestinal mucosa and cardiovascular system. Among the prostanoid receptors, the structure of antagonist-bound DP2, which belongs to the chemoattractant receptor family, was previously determined. However, the mechanisms of prostanoid recognition and receptor activation remained elusive. To address this issue, we determined the crystal structures of antagonist-bound EP4 and PGE2-bound EP3. The EP3-PGE2 complex exhibits an active-like conformation, including outward movement of the cytoplasmic end of transmembrane (TM) 6 relative to the cytoplasmic end of TM6 of the EP4 complex. The carboxyl moiety of PGE2 is recognized through three hydrogen bonds formed by highly conserved residues: Y1142.65, T206Extracelluar loop 2 (ECL2), and R3337.40 (superscripts denote Ballesteros-Weinstein numbering). In addition, the ω-chain of PGE2 orients toward TM6, which appears to contribute to receptor activation. The structure reveals important insights into the activation mechanism of prostanoid receptors and provides a molecular basis for the binding modes of endogenous ligands. These findings should facilitate the development of subtype-selective and non-PG-like ligands." @default.
- W3148296711 created "2021-04-13" @default.
- W3148296711 creator A5041986322 @default.
- W3148296711 date "2021-04-01" @default.
- W3148296711 modified "2023-09-27" @default.
- W3148296711 title "Activation Mechanism of Prostanoid Receptors —X-ray Crystallography of EP3 Receptor—" @default.
- W3148296711 doi "https://doi.org/10.1248/yakushi.20-00202" @default.
- W3148296711 hasPubMedId "https://pubmed.ncbi.nlm.nih.gov/33790113" @default.
- W3148296711 hasPublicationYear "2021" @default.
- W3148296711 type Work @default.
- W3148296711 sameAs 3148296711 @default.
- W3148296711 citedByCount "0" @default.
- W3148296711 crossrefType "journal-article" @default.
- W3148296711 hasAuthorship W3148296711A5041986322 @default.
- W3148296711 hasBestOaLocation W31482967111 @default.
- W3148296711 hasConcept C103474210 @default.
- W3148296711 hasConcept C135285700 @default.
- W3148296711 hasConcept C170493617 @default.
- W3148296711 hasConcept C178592051 @default.
- W3148296711 hasConcept C181199279 @default.
- W3148296711 hasConcept C185592680 @default.
- W3148296711 hasConcept C2778078955 @default.
- W3148296711 hasConcept C2778266237 @default.
- W3148296711 hasConcept C2778938600 @default.
- W3148296711 hasConcept C2780978440 @default.
- W3148296711 hasConcept C2781024287 @default.
- W3148296711 hasConcept C2909278008 @default.
- W3148296711 hasConcept C55493867 @default.
- W3148296711 hasConcept C86803240 @default.
- W3148296711 hasConcept C95444343 @default.
- W3148296711 hasConceptScore W3148296711C103474210 @default.
- W3148296711 hasConceptScore W3148296711C135285700 @default.
- W3148296711 hasConceptScore W3148296711C170493617 @default.
- W3148296711 hasConceptScore W3148296711C178592051 @default.
- W3148296711 hasConceptScore W3148296711C181199279 @default.
- W3148296711 hasConceptScore W3148296711C185592680 @default.
- W3148296711 hasConceptScore W3148296711C2778078955 @default.
- W3148296711 hasConceptScore W3148296711C2778266237 @default.
- W3148296711 hasConceptScore W3148296711C2778938600 @default.
- W3148296711 hasConceptScore W3148296711C2780978440 @default.
- W3148296711 hasConceptScore W3148296711C2781024287 @default.
- W3148296711 hasConceptScore W3148296711C2909278008 @default.
- W3148296711 hasConceptScore W3148296711C55493867 @default.
- W3148296711 hasConceptScore W3148296711C86803240 @default.
- W3148296711 hasConceptScore W3148296711C95444343 @default.
- W3148296711 hasIssue "4" @default.
- W3148296711 hasLocation W31482967111 @default.
- W3148296711 hasOpenAccess W3148296711 @default.
- W3148296711 hasPrimaryLocation W31482967111 @default.
- W3148296711 hasRelatedWork W169335434 @default.
- W3148296711 hasRelatedWork W183417552 @default.
- W3148296711 hasRelatedWork W1986338304 @default.
- W3148296711 hasRelatedWork W2013079253 @default.
- W3148296711 hasRelatedWork W2026908648 @default.
- W3148296711 hasRelatedWork W2055142026 @default.
- W3148296711 hasRelatedWork W2119466081 @default.
- W3148296711 hasRelatedWork W2419088265 @default.
- W3148296711 hasRelatedWork W2518776124 @default.
- W3148296711 hasRelatedWork W3147191058 @default.
- W3148296711 hasVolume "141" @default.
- W3148296711 isParatext "false" @default.
- W3148296711 isRetracted "false" @default.
- W3148296711 magId "3148296711" @default.
- W3148296711 workType "article" @default.