Matches in SemOpenAlex for { <https://semopenalex.org/work/W2013374553> ?p ?o ?g. }
Showing items 1 to 81 of
81
with 100 items per page.
- W2013374553 endingPage "537" @default.
- W2013374553 startingPage "536" @default.
- W2013374553 abstract "We report the crystallographic structures of the potent phosphoantigens Phosphostim (the bromohydrin of isopentenyl pyrophosphate) and E-4-hydroxy-3-methyl-but-2-enyl pyrophosphate bound to the mevalonate pathway enzyme isopentenyl pyrophosphate/dimethylallyl pyrophosphate isomerase (IPPI). Racemic Phosphostim forms covalent complexes with IPPI: a 4-thioether with C67 and a 4-ester with E116. Only the E116 ester forms with the chiral species, S-Phosphostim, with the w.t. enzyme, while the C67 thioether forms with a mutant Y104F IPPI. The potent phosphoantigen HMBPP also binds to IPPI, but is only a weak (∼50 μM) inhibitor. These results strongly support an SN2 reaction for inhibition of IPPI by Phosphostim, in contrast to the SN1 or concerted type of reaction found with epoxide inhibitors, which react at C-3, and are of general interest in the context of the development of novel mevalonate pathway inhibitors. They also provide clues as to the nature of the binding site of synthetic phosphoantigens in γδ T cell activation. In particular, both bromohydrin and epoxy phosphoantigens are potent, irreversible inhibitors of IPPI while HMBPP is only a weak inhibitor, ruling out an IPPI or IPPI-like target for HMBPP in γδ T cell activation." @default.
- W2013374553 created "2016-06-24" @default.
- W2013374553 creator A5004559759 @default.
- W2013374553 creator A5026780492 @default.
- W2013374553 creator A5032187402 @default.
- W2013374553 creator A5035735834 @default.
- W2013374553 creator A5049160817 @default.
- W2013374553 creator A5063163553 @default.
- W2013374553 creator A5080397665 @default.
- W2013374553 creator A5090566800 @default.
- W2013374553 creator A5090736392 @default.
- W2013374553 date "2004-12-23" @default.
- W2013374553 modified "2023-10-11" @default.
- W2013374553 title "A Crystallographic Investigation of Phosphoantigen Binding to Isopentenyl Pyrophosphate/Dimethylallyl Pyrophosphate Isomerase" @default.
- W2013374553 cites W1987608235 @default.
- W2013374553 cites W1999642437 @default.
- W2013374553 cites W2029667189 @default.
- W2013374553 cites W2036616071 @default.
- W2013374553 cites W2054508208 @default.
- W2013374553 cites W2107169184 @default.
- W2013374553 cites W2127367385 @default.
- W2013374553 cites W2170263258 @default.
- W2013374553 cites W2171736405 @default.
- W2013374553 cites W60551495 @default.
- W2013374553 doi "https://doi.org/10.1021/ja040207i" @default.
- W2013374553 hasPubMedId "https://pubmed.ncbi.nlm.nih.gov/15643873" @default.
- W2013374553 hasPublicationYear "2004" @default.
- W2013374553 type Work @default.
- W2013374553 sameAs 2013374553 @default.
- W2013374553 citedByCount "9" @default.
- W2013374553 countsByYear W20133745532013 @default.
- W2013374553 countsByYear W20133745532016 @default.
- W2013374553 countsByYear W20133745532017 @default.
- W2013374553 crossrefType "journal-article" @default.
- W2013374553 hasAuthorship W2013374553A5004559759 @default.
- W2013374553 hasAuthorship W2013374553A5026780492 @default.
- W2013374553 hasAuthorship W2013374553A5032187402 @default.
- W2013374553 hasAuthorship W2013374553A5035735834 @default.
- W2013374553 hasAuthorship W2013374553A5049160817 @default.
- W2013374553 hasAuthorship W2013374553A5063163553 @default.
- W2013374553 hasAuthorship W2013374553A5080397665 @default.
- W2013374553 hasAuthorship W2013374553A5090566800 @default.
- W2013374553 hasAuthorship W2013374553A5090736392 @default.
- W2013374553 hasConcept C181199279 @default.
- W2013374553 hasConcept C185592680 @default.
- W2013374553 hasConcept C2776043855 @default.
- W2013374553 hasConcept C2777654137 @default.
- W2013374553 hasConcept C2779444094 @default.
- W2013374553 hasConcept C2781264208 @default.
- W2013374553 hasConcept C55493867 @default.
- W2013374553 hasConcept C71240020 @default.
- W2013374553 hasConceptScore W2013374553C181199279 @default.
- W2013374553 hasConceptScore W2013374553C185592680 @default.
- W2013374553 hasConceptScore W2013374553C2776043855 @default.
- W2013374553 hasConceptScore W2013374553C2777654137 @default.
- W2013374553 hasConceptScore W2013374553C2779444094 @default.
- W2013374553 hasConceptScore W2013374553C2781264208 @default.
- W2013374553 hasConceptScore W2013374553C55493867 @default.
- W2013374553 hasConceptScore W2013374553C71240020 @default.
- W2013374553 hasIssue "2" @default.
- W2013374553 hasLocation W20133745531 @default.
- W2013374553 hasLocation W20133745532 @default.
- W2013374553 hasOpenAccess W2013374553 @default.
- W2013374553 hasPrimaryLocation W20133745531 @default.
- W2013374553 hasRelatedWork W1027211134 @default.
- W2013374553 hasRelatedWork W2006570241 @default.
- W2013374553 hasRelatedWork W2020386765 @default.
- W2013374553 hasRelatedWork W2091113436 @default.
- W2013374553 hasRelatedWork W2093651790 @default.
- W2013374553 hasRelatedWork W2196547254 @default.
- W2013374553 hasRelatedWork W2338527165 @default.
- W2013374553 hasRelatedWork W2344091048 @default.
- W2013374553 hasRelatedWork W2408936267 @default.
- W2013374553 hasRelatedWork W2531503415 @default.
- W2013374553 hasVolume "127" @default.
- W2013374553 isParatext "false" @default.
- W2013374553 isRetracted "false" @default.
- W2013374553 magId "2013374553" @default.
- W2013374553 workType "article" @default.