Matches in SemOpenAlex for { <https://semopenalex.org/work/W3190991590> ?p ?o ?g. }
- W3190991590 endingPage "1809" @default.
- W3190991590 startingPage "1798" @default.
- W3190991590 abstract "Identifying isoform-specific inhibitors for closely related kinase family members remains a substantial challenge. The necessity for achieving this specificity is exemplified by the RSK family, downstream effectors of ERK1/2, which have divergent physiological effects. The natural product, SL0101, a flavonoid glycoside, binds specifically to RSK1/2 through a binding pocket generated by an extensive conformational rearrangement within the RSK N-terminal kinase domain (NTKD). In modelling experiments a single amino acid that is divergent in RSK3/4 most likely prevents the required conformational rearrangement necessary for SL0101 binding. Kinetic analysis of RSK2 association with SL0101 and its derivatives identified that regions outside of the NTKD contribute to stable inhibitor binding. An analogue with an n-propyl-carbamate at the 4” position on the rhamnose moiety was identified that forms a highly stable inhibitor complex with RSK2 but not with RSK1. These results identify a SL0101 modification that will aid the identification of RSK2 specific inhibitors." @default.
- W3190991590 created "2021-08-16" @default.
- W3190991590 creator A5007146552 @default.
- W3190991590 creator A5008293667 @default.
- W3190991590 creator A5012698282 @default.
- W3190991590 creator A5018073672 @default.
- W3190991590 creator A5022584810 @default.
- W3190991590 creator A5076076931 @default.
- W3190991590 date "2021-01-01" @default.
- W3190991590 modified "2023-10-14" @default.
- W3190991590 title "Identifying requirements for RSK2 specific inhibitors" @default.
- W3190991590 cites W1471236775 @default.
- W3190991590 cites W1971593406 @default.
- W3190991590 cites W1988722937 @default.
- W3190991590 cites W1997746865 @default.
- W3190991590 cites W2001138775 @default.
- W3190991590 cites W2005002038 @default.
- W3190991590 cites W2016408686 @default.
- W3190991590 cites W2023747548 @default.
- W3190991590 cites W2033182904 @default.
- W3190991590 cites W2040473505 @default.
- W3190991590 cites W2042625441 @default.
- W3190991590 cites W2045815767 @default.
- W3190991590 cites W2046822015 @default.
- W3190991590 cites W2052615604 @default.
- W3190991590 cites W2089855272 @default.
- W3190991590 cites W2097349743 @default.
- W3190991590 cites W2114869204 @default.
- W3190991590 cites W2148210995 @default.
- W3190991590 cites W2151856174 @default.
- W3190991590 cites W2151931061 @default.
- W3190991590 cites W2153977062 @default.
- W3190991590 cites W2320719341 @default.
- W3190991590 cites W2469173987 @default.
- W3190991590 cites W2510331075 @default.
- W3190991590 cites W2551591409 @default.
- W3190991590 cites W2581729559 @default.
- W3190991590 cites W2587457642 @default.
- W3190991590 cites W2599780992 @default.
- W3190991590 cites W2608864033 @default.
- W3190991590 cites W2623191882 @default.
- W3190991590 cites W2797681865 @default.
- W3190991590 cites W2801491392 @default.
- W3190991590 cites W2807674960 @default.
- W3190991590 cites W2888098711 @default.
- W3190991590 cites W2916967884 @default.
- W3190991590 cites W3004054709 @default.
- W3190991590 cites W3088763490 @default.
- W3190991590 doi "https://doi.org/10.1080/14756366.2021.1957862" @default.
- W3190991590 hasPubMedCentralId "https://www.ncbi.nlm.nih.gov/pmc/articles/8344253" @default.
- W3190991590 hasPubMedId "https://pubmed.ncbi.nlm.nih.gov/34348556" @default.
- W3190991590 hasPublicationYear "2021" @default.
- W3190991590 type Work @default.
- W3190991590 sameAs 3190991590 @default.
- W3190991590 citedByCount "3" @default.
- W3190991590 countsByYear W31909915902022 @default.
- W3190991590 countsByYear W31909915902023 @default.
- W3190991590 crossrefType "journal-article" @default.
- W3190991590 hasAuthorship W3190991590A5007146552 @default.
- W3190991590 hasAuthorship W3190991590A5008293667 @default.
- W3190991590 hasAuthorship W3190991590A5012698282 @default.
- W3190991590 hasAuthorship W3190991590A5018073672 @default.
- W3190991590 hasAuthorship W3190991590A5022584810 @default.
- W3190991590 hasAuthorship W3190991590A5076076931 @default.
- W3190991590 hasBestOaLocation W31909915901 @default.
- W3190991590 hasConcept C104317684 @default.
- W3190991590 hasConcept C107824862 @default.
- W3190991590 hasConcept C184235292 @default.
- W3190991590 hasConcept C185592680 @default.
- W3190991590 hasConcept C2776568683 @default.
- W3190991590 hasConcept C2779396153 @default.
- W3190991590 hasConcept C3020299119 @default.
- W3190991590 hasConcept C51785407 @default.
- W3190991590 hasConcept C53345823 @default.
- W3190991590 hasConcept C55493867 @default.
- W3190991590 hasConcept C70721500 @default.
- W3190991590 hasConcept C71240020 @default.
- W3190991590 hasConcept C86803240 @default.
- W3190991590 hasConceptScore W3190991590C104317684 @default.
- W3190991590 hasConceptScore W3190991590C107824862 @default.
- W3190991590 hasConceptScore W3190991590C184235292 @default.
- W3190991590 hasConceptScore W3190991590C185592680 @default.
- W3190991590 hasConceptScore W3190991590C2776568683 @default.
- W3190991590 hasConceptScore W3190991590C2779396153 @default.
- W3190991590 hasConceptScore W3190991590C3020299119 @default.
- W3190991590 hasConceptScore W3190991590C51785407 @default.
- W3190991590 hasConceptScore W3190991590C53345823 @default.
- W3190991590 hasConceptScore W3190991590C55493867 @default.
- W3190991590 hasConceptScore W3190991590C70721500 @default.
- W3190991590 hasConceptScore W3190991590C71240020 @default.
- W3190991590 hasConceptScore W3190991590C86803240 @default.
- W3190991590 hasFunder F4320306076 @default.
- W3190991590 hasFunder F4320332161 @default.
- W3190991590 hasIssue "1" @default.
- W3190991590 hasLocation W31909915901 @default.
- W3190991590 hasLocation W31909915902 @default.
- W3190991590 hasLocation W31909915903 @default.
- W3190991590 hasLocation W31909915904 @default.