FRINK Linked Data Fragments server

Matches in SemOpenAlex for { <https://semopenalex.org/work/W2974006918> ?p ?o ?g. }

• W2974006918 endingPage "533" @default.
• W2974006918 startingPage "521" @default.
• W2974006918 abstract "Objective: Prostaglandin 2 (PGD2) mediated signalling of Chemoattractant Receptorhomologous molecule expressed on Th2 cells (CRTh2) receptor has been implicated in the recruitment of inflammatory cells. This explains the design of highly selective compounds with innate abilities to antagonize PGD2-CRTh2 interactions and prevent pro-inflammatory allergies such as rhinitis and uncontrolled asthma. The development of PGD2-competitive CRTh2 binders; CAY10471 and Fevipiprant represent remarkable therapeutic progress even though they elicit disparate pharmacological propensities despite utilizing the same binding pocket. Methods & Results: In this study, we seek to pinpoint the underlying phenomenon associated with differential CRTh2 therapeutic inhibition by CAY10471 and Fevipiprant using membraneembedded molecular dynamics simulation. Findings revealed that the common carboxylate group of both compounds elicited strong attractive charges with active site Arg170 and Lys210. Interestingly, a distinctive feature was the steady occurrence of high-affinity salt-bridges and an Arg170-mediated pi-cation interaction with the tetrahydrocarbozole ring of CAY10471. Further investigations into the active site motions of both ligands revealed that CAY10471 was relatively more stable. Comparative binding analyses also revealed that CAY10471 exhibited higher ΔG, indicating the cruciality of the ring stabilization role mediated by Arg170. Moreover, conformational analyses revealed that the inhibitory activity of CAY10471 was more prominent on CRTh2 compared to Fevipiprant. Conclusion: These findings could further advance the strategic design of novel CRTh2 binders in the treatment of diseases related to pro-inflammatory allergies." @default.
• W2974006918 created "2019-09-26" @default.
• W2974006918 creator A5021219358 @default.
• W2974006918 creator A5030380866 @default.
• W2974006918 creator A5035779221 @default.
• W2974006918 creator A5044280726 @default.
• W2974006918 creator A5070955314 @default.
• W2974006918 creator A5075199070 @default.
• W2974006918 creator A5086232993 @default.
• W2974006918 date "2019-12-19" @default.
• W2974006918 modified "2023-09-27" @default.
• W2974006918 title "Same Target, Different Therapeutic Outcomes: The Case of CAY10471 and Fevipiprant on CRTh2 Receptor in Treatment of Allergic Rhinitis and Asthma" @default.
• W2974006918 cites W1483555207 @default.
• W2974006918 cites W1491383197 @default.
• W2974006918 cites W1512168554 @default.
• W2974006918 cites W1519407136 @default.
• W2974006918 cites W1968984443 @default.
• W2974006918 cites W1969900280 @default.
• W2974006918 cites W1976499671 @default.
• W2974006918 cites W1985242752 @default.
• W2974006918 cites W2018464738 @default.
• W2974006918 cites W2020627803 @default.
• W2974006918 cites W2037961164 @default.
• W2974006918 cites W2053894571 @default.
• W2974006918 cites W2066882388 @default.
• W2974006918 cites W2073939652 @default.
• W2974006918 cites W2097775366 @default.
• W2974006918 cites W2099886404 @default.
• W2974006918 cites W2100705331 @default.
• W2974006918 cites W2116105539 @default.
• W2974006918 cites W2124251887 @default.
• W2974006918 cites W2128382611 @default.
• W2974006918 cites W2131032941 @default.
• W2974006918 cites W2140688081 @default.
• W2974006918 cites W2150068375 @default.
• W2974006918 cites W2166893697 @default.
• W2974006918 cites W2172874896 @default.
• W2974006918 cites W2297115086 @default.
• W2974006918 cites W2313856416 @default.
• W2974006918 cites W2323104785 @default.
• W2974006918 cites W2328479868 @default.
• W2974006918 cites W2404280981 @default.
• W2974006918 cites W2471862159 @default.
• W2974006918 cites W2475158269 @default.
• W2974006918 cites W2510774880 @default.
• W2974006918 cites W2590271258 @default.
• W2974006918 cites W2608159180 @default.
• W2974006918 cites W2625270096 @default.
• W2974006918 cites W2745578669 @default.
• W2974006918 cites W2773377402 @default.
• W2974006918 cites W2783351753 @default.
• W2974006918 cites W2791453916 @default.
• W2974006918 cites W2810272478 @default.
• W2974006918 cites W2891161399 @default.
• W2974006918 cites W2906821479 @default.
• W2974006918 cites W2908121480 @default.
• W2974006918 doi "https://doi.org/10.2174/1386207322666190919113006" @default.
• W2974006918 hasPubMedId "https://pubmed.ncbi.nlm.nih.gov/31538888" @default.
• W2974006918 hasPublicationYear "2019" @default.
• W2974006918 type Work @default.
• W2974006918 sameAs 2974006918 @default.
• W2974006918 citedByCount "6" @default.
• W2974006918 countsByYear W29740069182020 @default.
• W2974006918 countsByYear W29740069182022 @default.
• W2974006918 countsByYear W29740069182023 @default.
• W2974006918 crossrefType "journal-article" @default.
• W2974006918 hasAuthorship W2974006918A5021219358 @default.
• W2974006918 hasAuthorship W2974006918A5030380866 @default.
• W2974006918 hasAuthorship W2974006918A5035779221 @default.
• W2974006918 hasAuthorship W2974006918A5044280726 @default.
• W2974006918 hasAuthorship W2974006918A5070955314 @default.
• W2974006918 hasAuthorship W2974006918A5075199070 @default.
• W2974006918 hasAuthorship W2974006918A5086232993 @default.
• W2974006918 hasConcept C126322002 @default.
• W2974006918 hasConcept C161624437 @default.
• W2974006918 hasConcept C170493617 @default.
• W2974006918 hasConcept C17077164 @default.
• W2974006918 hasConcept C185592680 @default.
• W2974006918 hasConcept C203014093 @default.
• W2974006918 hasConcept C207480886 @default.
• W2974006918 hasConcept C2776042228 @default.
• W2974006918 hasConcept C54166955 @default.
• W2974006918 hasConcept C55493867 @default.
• W2974006918 hasConcept C71924100 @default.
• W2974006918 hasConceptScore W2974006918C126322002 @default.
• W2974006918 hasConceptScore W2974006918C161624437 @default.
• W2974006918 hasConceptScore W2974006918C170493617 @default.
• W2974006918 hasConceptScore W2974006918C17077164 @default.
• W2974006918 hasConceptScore W2974006918C185592680 @default.
• W2974006918 hasConceptScore W2974006918C203014093 @default.
• W2974006918 hasConceptScore W2974006918C207480886 @default.
• W2974006918 hasConceptScore W2974006918C2776042228 @default.
• W2974006918 hasConceptScore W2974006918C54166955 @default.
• W2974006918 hasConceptScore W2974006918C55493867 @default.
• W2974006918 hasConceptScore W2974006918C71924100 @default.
• W2974006918 hasIssue "8" @default.
• W2974006918 hasLocation W29740069181 @default.
• W2974006918 hasLocation W29740069182 @default.

• next