Matches in SemOpenAlex for { <https://semopenalex.org/work/W2014333071> ?p ?o ?g. }
- W2014333071 endingPage "458" @default.
- W2014333071 startingPage "451" @default.
- W2014333071 abstract "Caspase-1 is a key endopeptidase responsible for the post-translational processing of the IL-1beta and IL-18 cytokines and small-molecule inhibitors that modulate the activity of this enzyme are predicted to be important therapeutic treatments for many inflammatory diseases. A fragment-assembly approach, accompanied by structural analysis, was employed to generate caspase-1 inhibitors. With the aid of Tethering with extenders (small molecules that bind to the active-site cysteine and contain a free thiol), two novel fragments that bound to the active site and made a disulfide bond with the extender were identified by mass spectrometry. Direct linking of each fragment to the extender generated submicromolar reversible inhibitors that significantly reduced secretion of IL-1beta but not IL-6 from human peripheral blood mononuclear cells. Thus, Tethering with extenders facilitated rapid identification and synthesis of caspase-1 inhibitors with cell-based activity and subsequent structural analyses provided insights into the enzyme's ability to accommodate different inhibitor-binding modes in the active site." @default.
- W2014333071 created "2016-06-24" @default.
- W2014333071 creator A5012257984 @default.
- W2014333071 creator A5018363968 @default.
- W2014333071 creator A5028797169 @default.
- W2014333071 creator A5036312982 @default.
- W2014333071 creator A5043150666 @default.
- W2014333071 creator A5043250044 @default.
- W2014333071 creator A5052941291 @default.
- W2014333071 creator A5059487957 @default.
- W2014333071 creator A5072333119 @default.
- W2014333071 date "2005-04-09" @default.
- W2014333071 modified "2023-10-18" @default.
- W2014333071 title "Structural analysis of caspase-1 inhibitors derived from Tethering" @default.
- W2014333071 cites W1529674879 @default.
- W2014333071 cites W1921587687 @default.
- W2014333071 cites W1933988754 @default.
- W2014333071 cites W1958466825 @default.
- W2014333071 cites W1964977785 @default.
- W2014333071 cites W1983611229 @default.
- W2014333071 cites W1984338631 @default.
- W2014333071 cites W1999590520 @default.
- W2014333071 cites W2008261126 @default.
- W2014333071 cites W2009073915 @default.
- W2014333071 cites W2013083986 @default.
- W2014333071 cites W2016255772 @default.
- W2014333071 cites W2024105041 @default.
- W2014333071 cites W2036005030 @default.
- W2014333071 cites W2038840577 @default.
- W2014333071 cites W205138462 @default.
- W2014333071 cites W2051658957 @default.
- W2014333071 cites W2052895824 @default.
- W2014333071 cites W2053718635 @default.
- W2014333071 cites W2066349847 @default.
- W2014333071 cites W2072944243 @default.
- W2014333071 cites W2087092800 @default.
- W2014333071 cites W2088686292 @default.
- W2014333071 cites W2089154951 @default.
- W2014333071 cites W2100075779 @default.
- W2014333071 cites W2105091660 @default.
- W2014333071 cites W2105263387 @default.
- W2014333071 cites W2114266096 @default.
- W2014333071 cites W2116947993 @default.
- W2014333071 cites W2126144943 @default.
- W2014333071 cites W2127314810 @default.
- W2014333071 cites W2138958920 @default.
- W2014333071 cites W2141380905 @default.
- W2014333071 cites W2149605526 @default.
- W2014333071 cites W61910122 @default.
- W2014333071 doi "https://doi.org/10.1107/s1744309105010109" @default.
- W2014333071 hasPubMedCentralId "https://www.ncbi.nlm.nih.gov/pmc/articles/1952309" @default.
- W2014333071 hasPubMedId "https://pubmed.ncbi.nlm.nih.gov/16511067" @default.
- W2014333071 hasPublicationYear "2005" @default.
- W2014333071 type Work @default.
- W2014333071 sameAs 2014333071 @default.
- W2014333071 citedByCount "21" @default.
- W2014333071 countsByYear W20143330712012 @default.
- W2014333071 countsByYear W20143330712014 @default.
- W2014333071 countsByYear W20143330712015 @default.
- W2014333071 countsByYear W20143330712018 @default.
- W2014333071 countsByYear W20143330712019 @default.
- W2014333071 countsByYear W20143330712022 @default.
- W2014333071 countsByYear W20143330712023 @default.
- W2014333071 crossrefType "journal-article" @default.
- W2014333071 hasAuthorship W2014333071A5012257984 @default.
- W2014333071 hasAuthorship W2014333071A5018363968 @default.
- W2014333071 hasAuthorship W2014333071A5028797169 @default.
- W2014333071 hasAuthorship W2014333071A5036312982 @default.
- W2014333071 hasAuthorship W2014333071A5043150666 @default.
- W2014333071 hasAuthorship W2014333071A5043250044 @default.
- W2014333071 hasAuthorship W2014333071A5052941291 @default.
- W2014333071 hasAuthorship W2014333071A5059487957 @default.
- W2014333071 hasAuthorship W2014333071A5072333119 @default.
- W2014333071 hasBestOaLocation W20143330712 @default.
- W2014333071 hasConcept C107824862 @default.
- W2014333071 hasConcept C137061746 @default.
- W2014333071 hasConcept C161624437 @default.
- W2014333071 hasConcept C181199279 @default.
- W2014333071 hasConcept C185592680 @default.
- W2014333071 hasConcept C201815810 @default.
- W2014333071 hasConcept C202751555 @default.
- W2014333071 hasConcept C2779201268 @default.
- W2014333071 hasConcept C41183919 @default.
- W2014333071 hasConcept C55493867 @default.
- W2014333071 hasConcept C71240020 @default.
- W2014333071 hasConcept C86803240 @default.
- W2014333071 hasConcept C95444343 @default.
- W2014333071 hasConceptScore W2014333071C107824862 @default.
- W2014333071 hasConceptScore W2014333071C137061746 @default.
- W2014333071 hasConceptScore W2014333071C161624437 @default.
- W2014333071 hasConceptScore W2014333071C181199279 @default.
- W2014333071 hasConceptScore W2014333071C185592680 @default.
- W2014333071 hasConceptScore W2014333071C201815810 @default.
- W2014333071 hasConceptScore W2014333071C202751555 @default.
- W2014333071 hasConceptScore W2014333071C2779201268 @default.
- W2014333071 hasConceptScore W2014333071C41183919 @default.
- W2014333071 hasConceptScore W2014333071C55493867 @default.
- W2014333071 hasConceptScore W2014333071C71240020 @default.