Matches in SemOpenAlex for { <https://semopenalex.org/work/W4220865087> ?p ?o ?g. }
Showing items 1 to 90 of
90
with 100 items per page.
- W4220865087 endingPage "40" @default.
- W4220865087 startingPage "25" @default.
- W4220865087 abstract "Sigma receptor is a transmembrane non-GPCR protein expressed mainly in the endoplasmic reticulum membrane associated with mitochondria. It is classified into two types: Sigma-1 (S1R) and Sigma-2 (S2R) based on their biological functions. S1R has been implicated in many neurological disorders such as anxiety, schizophrenia, and depression. Therefore, S1R ligands possess a variety of potential clinical applications with a great interest in the treatment of neuropathic pain. In this study, we report the discovery of a novel lead compound for S1R binding, based on the thiazolidine-2,4-dione nucleus. We have explored hydrophobic groups of different sizes on both sides of the five-membered ring scaffold guided by the crystal structure of S1R. Six compounds showed more than 50% displacement of the radioligand at 10 µM concentration with compound 6c resulting in 100% displacement and a Ki of 95.5 nM. Moreover, compounds 6c and 6e showed a significant selectivity over S2R. In addition, molecular docking predicted that all the compounds showed the critical salt bridge with Glu172 with variable degrees of π-stacking interaction with Tyr103. Upon optimization, this series of compounds could represent potential clinically useful S1R ligands for pain management." @default.
- W4220865087 created "2022-04-03" @default.
- W4220865087 creator A5003045933 @default.
- W4220865087 creator A5003657695 @default.
- W4220865087 creator A5010239913 @default.
- W4220865087 creator A5022235285 @default.
- W4220865087 creator A5046736185 @default.
- W4220865087 creator A5046760541 @default.
- W4220865087 creator A5053896803 @default.
- W4220865087 creator A5060937233 @default.
- W4220865087 date "2022-04-25" @default.
- W4220865087 modified "2023-09-27" @default.
- W4220865087 title "Discovery of 3‐(2‐aminoethyl)‐thiazolidine‐2,4‐diones as a novel chemotype of sigma‐1 receptor ligands" @default.
- W4220865087 cites W1979600197 @default.
- W4220865087 cites W2015772507 @default.
- W4220865087 cites W2027616377 @default.
- W4220865087 cites W2043509228 @default.
- W4220865087 cites W2067643341 @default.
- W4220865087 cites W2314811232 @default.
- W4220865087 cites W2315207226 @default.
- W4220865087 cites W2315469262 @default.
- W4220865087 cites W2338034663 @default.
- W4220865087 cites W2396930286 @default.
- W4220865087 cites W2564690222 @default.
- W4220865087 cites W2593436234 @default.
- W4220865087 cites W2614102372 @default.
- W4220865087 cites W2618221287 @default.
- W4220865087 cites W2734381060 @default.
- W4220865087 cites W2792482118 @default.
- W4220865087 cites W2801088198 @default.
- W4220865087 cites W2887837938 @default.
- W4220865087 cites W2951156176 @default.
- W4220865087 cites W3151444381 @default.
- W4220865087 cites W3161654284 @default.
- W4220865087 cites W3162134450 @default.
- W4220865087 cites W3164253088 @default.
- W4220865087 cites W3169315007 @default.
- W4220865087 cites W3175725064 @default.
- W4220865087 doi "https://doi.org/10.1111/cbdd.14047" @default.
- W4220865087 hasPubMedId "https://pubmed.ncbi.nlm.nih.gov/35353926" @default.
- W4220865087 hasPublicationYear "2022" @default.
- W4220865087 type Work @default.
- W4220865087 citedByCount "4" @default.
- W4220865087 countsByYear W42208650872022 @default.
- W4220865087 countsByYear W42208650872023 @default.
- W4220865087 crossrefType "journal-article" @default.
- W4220865087 hasAuthorship W4220865087A5003045933 @default.
- W4220865087 hasAuthorship W4220865087A5003657695 @default.
- W4220865087 hasAuthorship W4220865087A5010239913 @default.
- W4220865087 hasAuthorship W4220865087A5022235285 @default.
- W4220865087 hasAuthorship W4220865087A5046736185 @default.
- W4220865087 hasAuthorship W4220865087A5046760541 @default.
- W4220865087 hasAuthorship W4220865087A5053896803 @default.
- W4220865087 hasAuthorship W4220865087A5060937233 @default.
- W4220865087 hasConcept C103133801 @default.
- W4220865087 hasConcept C170493617 @default.
- W4220865087 hasConcept C185592680 @default.
- W4220865087 hasConcept C2778938600 @default.
- W4220865087 hasConcept C55493867 @default.
- W4220865087 hasConcept C67847695 @default.
- W4220865087 hasConcept C71240020 @default.
- W4220865087 hasConceptScore W4220865087C103133801 @default.
- W4220865087 hasConceptScore W4220865087C170493617 @default.
- W4220865087 hasConceptScore W4220865087C185592680 @default.
- W4220865087 hasConceptScore W4220865087C2778938600 @default.
- W4220865087 hasConceptScore W4220865087C55493867 @default.
- W4220865087 hasConceptScore W4220865087C67847695 @default.
- W4220865087 hasConceptScore W4220865087C71240020 @default.
- W4220865087 hasFunder F4320321116 @default.
- W4220865087 hasIssue "1" @default.
- W4220865087 hasLocation W42208650871 @default.
- W4220865087 hasLocation W42208650872 @default.
- W4220865087 hasOpenAccess W4220865087 @default.
- W4220865087 hasPrimaryLocation W42208650871 @default.
- W4220865087 hasRelatedWork W1960147035 @default.
- W4220865087 hasRelatedWork W1970907396 @default.
- W4220865087 hasRelatedWork W2033854365 @default.
- W4220865087 hasRelatedWork W2055397294 @default.
- W4220865087 hasRelatedWork W2075285753 @default.
- W4220865087 hasRelatedWork W2085878653 @default.
- W4220865087 hasRelatedWork W2168015511 @default.
- W4220865087 hasRelatedWork W2248429942 @default.
- W4220865087 hasRelatedWork W2470122678 @default.
- W4220865087 hasRelatedWork W2773157959 @default.
- W4220865087 hasVolume "100" @default.
- W4220865087 isParatext "false" @default.
- W4220865087 isRetracted "false" @default.
- W4220865087 workType "article" @default.