FRINK Linked Data Fragments server

Matches in SemOpenAlex for { <https://semopenalex.org/work/W1550129999> ?p ?o ?g. }

• W1550129999 endingPage "1439" @default.
• W1550129999 startingPage "1429" @default.
• W1550129999 abstract "Background and purpose: We have previously shown that SB265610 (1‐(2‐bromo‐phenyl)‐3‐(7‐cyano‐3H‐benzotriazol‐4‐yl)‐urea) behaves as an allosteric, inverse agonist at the C‐X‐C chemokine (CXCR)2 receptor. The aim of this study was to determine whether SB265610, in addition to two other known antagonists, bind to either of the two putative, topographically distinct, allosteric binding sites previously reported in the Literature. Experimental approach: Ten single point mutations were introduced into the CXCR2 receptor using site‐directed mutagenesis. Three CXCR2 antagonists were investigated, SB265610, Pteridone‐1 (2‐(2,3 difluoro‐benzylsulphanyl)‐4‐((R)‐2‐hydroxy‐1‐methyl‐ethylamino)‐8H‐pteridin‐7‐one) and Sch527123 (2‐hydroxy‐N,N‐dimethyl‐3‐{2‐[[(R)‐1‐(5‐methyl‐furan‐2‐yl)‐propyl]amino]‐3,4‐dioxo‐cyclobut‐1enylamino}‐benzamide), and the effect of these mutations on their binding affinity and ability to inhibit interleukin‐8‐stimulated binding of [ 35 S]GTPγS was examined. Key results: Seven of the nine mutations introduced into the C‐terminal domain and intracellular loops of the receptor produced a significant reduction in affinity at least one of the antagonists tested. Of those seven mutations, three produced a significant reduction in the affinity of all three antagonists, namely K320A, Y314A and D84N. In all but one mutation, the changes observed on antagonist affinity were matched with effects on inhibition of interleukin‐8‐stimulated [ 35 S]GTPγS binding. Conclusions and implications: These antagonists bind to a common intracellular, allosteric, binding site of the CXCR2 receptor, which has been further delineated. As many of these mutations are close to the site of G protein coupling or to a region of the receptor that is responsible for the transduction of the activation signal, our results suggest a molecular mechanism for the inhibition of receptor activation." @default.
• W1550129999 created "2016-06-24" @default.
• W1550129999 creator A5015047364 @default.
• W1550129999 creator A5016588034 @default.
• W1550129999 creator A5028902996 @default.
• W1550129999 creator A5040052707 @default.
• W1550129999 creator A5041399508 @default.
• W1550129999 creator A5053966934 @default.
• W1550129999 creator A5072002217 @default.
• W1550129999 date "2010-03-22" @default.
• W1550129999 modified "2023-10-18" @default.
• W1550129999 title "A common intracellular allosteric binding site for antagonists of the CXCR2 receptor" @default.
• W1550129999 cites W1549683321 @default.
• W1550129999 cites W1933354778 @default.
• W1550129999 cites W1944281814 @default.
• W1550129999 cites W1988019968 @default.
• W1550129999 cites W2020548323 @default.
• W1550129999 cites W2024040954 @default.
• W1550129999 cites W2044809386 @default.
• W1550129999 cites W2060963460 @default.
• W1550129999 cites W2069380892 @default.
• W1550129999 cites W2078901618 @default.
• W1550129999 cites W2081381389 @default.
• W1550129999 cites W2085381168 @default.
• W1550129999 cites W2088124775 @default.
• W1550129999 cites W2089780525 @default.
• W1550129999 cites W2136836360 @default.
• W1550129999 cites W2139945041 @default.
• W1550129999 cites W2155546261 @default.
• W1550129999 cites W4231241402 @default.
• W1550129999 doi "https://doi.org/10.1111/j.1476-5381.2009.00623.x" @default.
• W1550129999 hasPubMedCentralId "https://www.ncbi.nlm.nih.gov/pmc/articles/2850400" @default.
• W1550129999 hasPubMedId "https://pubmed.ncbi.nlm.nih.gov/20233217" @default.
• W1550129999 hasPublicationYear "2010" @default.
• W1550129999 type Work @default.
• W1550129999 sameAs 1550129999 @default.
• W1550129999 citedByCount "71" @default.
• W1550129999 countsByYear W15501299992012 @default.
• W1550129999 countsByYear W15501299992013 @default.
• W1550129999 countsByYear W15501299992014 @default.
• W1550129999 countsByYear W15501299992015 @default.
• W1550129999 countsByYear W15501299992016 @default.
• W1550129999 countsByYear W15501299992017 @default.
• W1550129999 countsByYear W15501299992018 @default.
• W1550129999 countsByYear W15501299992019 @default.
• W1550129999 countsByYear W15501299992020 @default.
• W1550129999 countsByYear W15501299992021 @default.
• W1550129999 countsByYear W15501299992022 @default.
• W1550129999 countsByYear W15501299992023 @default.
• W1550129999 crossrefType "journal-article" @default.
• W1550129999 hasAuthorship W1550129999A5015047364 @default.
• W1550129999 hasAuthorship W1550129999A5016588034 @default.
• W1550129999 hasAuthorship W1550129999A5028902996 @default.
• W1550129999 hasAuthorship W1550129999A5040052707 @default.
• W1550129999 hasAuthorship W1550129999A5041399508 @default.
• W1550129999 hasAuthorship W1550129999A5053966934 @default.
• W1550129999 hasAuthorship W1550129999A5072002217 @default.
• W1550129999 hasBestOaLocation W15501299992 @default.
• W1550129999 hasConcept C107824862 @default.
• W1550129999 hasConcept C118716 @default.
• W1550129999 hasConcept C166342909 @default.
• W1550129999 hasConcept C170493617 @default.
• W1550129999 hasConcept C181199279 @default.
• W1550129999 hasConcept C185592680 @default.
• W1550129999 hasConcept C2776885963 @default.
• W1550129999 hasConcept C2778938600 @default.
• W1550129999 hasConcept C55493867 @default.
• W1550129999 hasConcept C71240020 @default.
• W1550129999 hasConcept C79879829 @default.
• W1550129999 hasConcept C86803240 @default.
• W1550129999 hasConcept C98274493 @default.
• W1550129999 hasConceptScore W1550129999C107824862 @default.
• W1550129999 hasConceptScore W1550129999C118716 @default.
• W1550129999 hasConceptScore W1550129999C166342909 @default.
• W1550129999 hasConceptScore W1550129999C170493617 @default.
• W1550129999 hasConceptScore W1550129999C181199279 @default.
• W1550129999 hasConceptScore W1550129999C185592680 @default.
• W1550129999 hasConceptScore W1550129999C2776885963 @default.
• W1550129999 hasConceptScore W1550129999C2778938600 @default.
• W1550129999 hasConceptScore W1550129999C55493867 @default.
• W1550129999 hasConceptScore W1550129999C71240020 @default.
• W1550129999 hasConceptScore W1550129999C79879829 @default.
• W1550129999 hasConceptScore W1550129999C86803240 @default.
• W1550129999 hasConceptScore W1550129999C98274493 @default.
• W1550129999 hasIssue "7" @default.
• W1550129999 hasLocation W15501299991 @default.
• W1550129999 hasLocation W15501299992 @default.
• W1550129999 hasLocation W15501299993 @default.
• W1550129999 hasLocation W15501299994 @default.
• W1550129999 hasOpenAccess W1550129999 @default.
• W1550129999 hasPrimaryLocation W15501299991 @default.
• W1550129999 hasRelatedWork W1971782741 @default.
• W1550129999 hasRelatedWork W1979020445 @default.
• W1550129999 hasRelatedWork W2033181528 @default.
• W1550129999 hasRelatedWork W2046450796 @default.
• W1550129999 hasRelatedWork W2114161702 @default.
• W1550129999 hasRelatedWork W2125471807 @default.
• W1550129999 hasRelatedWork W2169750653 @default.

• next