Matches in SemOpenAlex for { <https://semopenalex.org/work/W4310641805> ?p ?o ?g. }
- W4310641805 abstract "Abstract Glycosyltransferases are a superfamily of enzymes that are notoriously difficult to inhibit. Here we apply an mRNA display technology integrated with genetic code reprogramming, referred to as the RaPID (random non‐standard peptides integrated discovery) system, to identify macrocyclic peptides with high binding affinities for O‐GlcNAc transferase (OGT). These macrocycles inhibit OGT activity through an allosteric mechanism that is driven by their binding to the tetratricopeptide repeats of OGT. Saturation mutagenesis in a maturation screen using 39 amino acids, including 22 non‐canonical residues, led to an improved unnatural macrocycle that is ≈40 times more potent than the parent compound ( K i app =1.5 nM). Subsequent derivatization delivered a biotinylated derivative that enabled one‐step affinity purification of OGT from complex samples. The high potency and novel mechanism of action of these OGT ligands should enable new approaches to elucidate the specificity and regulation of OGT." @default.
- W4310641805 created "2022-12-13" @default.
- W4310641805 creator A5009478169 @default.
- W4310641805 creator A5017224243 @default.
- W4310641805 creator A5036824067 @default.
- W4310641805 creator A5037200154 @default.
- W4310641805 creator A5053072115 @default.
- W4310641805 creator A5063389971 @default.
- W4310641805 creator A5072224327 @default.
- W4310641805 creator A5078248083 @default.
- W4310641805 date "2022-12-27" @default.
- W4310641805 modified "2023-10-17" @default.
- W4310641805 title "Potent De Novo Macrocyclic Peptides That Inhibit O‐GlcNAc Transferase through an Allosteric Mechanism" @default.
- W4310641805 cites W1997087248 @default.
- W4310641805 cites W1998906741 @default.
- W4310641805 cites W2000106654 @default.
- W4310641805 cites W2008832722 @default.
- W4310641805 cites W2016181996 @default.
- W4310641805 cites W2024591818 @default.
- W4310641805 cites W2040714286 @default.
- W4310641805 cites W2050775180 @default.
- W4310641805 cites W2060744329 @default.
- W4310641805 cites W2070666853 @default.
- W4310641805 cites W2072135796 @default.
- W4310641805 cites W2077451485 @default.
- W4310641805 cites W2079492290 @default.
- W4310641805 cites W2080462728 @default.
- W4310641805 cites W2087181770 @default.
- W4310641805 cites W2154249927 @default.
- W4310641805 cites W2158001771 @default.
- W4310641805 cites W2163107762 @default.
- W4310641805 cites W2257564321 @default.
- W4310641805 cites W2464384284 @default.
- W4310641805 cites W2507874699 @default.
- W4310641805 cites W2532344138 @default.
- W4310641805 cites W2544215763 @default.
- W4310641805 cites W2568160334 @default.
- W4310641805 cites W2603194836 @default.
- W4310641805 cites W2604618525 @default.
- W4310641805 cites W2616169167 @default.
- W4310641805 cites W2730056431 @default.
- W4310641805 cites W2789760611 @default.
- W4310641805 cites W2801169841 @default.
- W4310641805 cites W2804899379 @default.
- W4310641805 cites W2895737508 @default.
- W4310641805 cites W2896287573 @default.
- W4310641805 cites W2949015502 @default.
- W4310641805 cites W2971696841 @default.
- W4310641805 cites W2979778107 @default.
- W4310641805 cites W2998628971 @default.
- W4310641805 cites W3006886971 @default.
- W4310641805 cites W3040450164 @default.
- W4310641805 cites W3047310275 @default.
- W4310641805 cites W3122156717 @default.
- W4310641805 cites W3127884649 @default.
- W4310641805 cites W3158152080 @default.
- W4310641805 cites W3211889529 @default.
- W4310641805 cites W3217216416 @default.
- W4310641805 cites W4210531704 @default.
- W4310641805 cites W4229028232 @default.
- W4310641805 cites W4232695249 @default.
- W4310641805 cites W4245473379 @default.
- W4310641805 cites W4254135320 @default.
- W4310641805 cites W4281888381 @default.
- W4310641805 cites W4291652132 @default.
- W4310641805 cites W4293461777 @default.
- W4310641805 cites W4297373458 @default.
- W4310641805 doi "https://doi.org/10.1002/anie.202215671" @default.
- W4310641805 hasPubMedId "https://pubmed.ncbi.nlm.nih.gov/36460613" @default.
- W4310641805 hasPublicationYear "2022" @default.
- W4310641805 type Work @default.
- W4310641805 citedByCount "5" @default.
- W4310641805 countsByYear W43106418052023 @default.
- W4310641805 crossrefType "journal-article" @default.
- W4310641805 hasAuthorship W4310641805A5009478169 @default.
- W4310641805 hasAuthorship W4310641805A5017224243 @default.
- W4310641805 hasAuthorship W4310641805A5036824067 @default.
- W4310641805 hasAuthorship W4310641805A5037200154 @default.
- W4310641805 hasAuthorship W4310641805A5053072115 @default.
- W4310641805 hasAuthorship W4310641805A5063389971 @default.
- W4310641805 hasAuthorship W4310641805A5072224327 @default.
- W4310641805 hasAuthorship W4310641805A5078248083 @default.
- W4310641805 hasConcept C104317684 @default.
- W4310641805 hasConcept C161019410 @default.
- W4310641805 hasConcept C16318435 @default.
- W4310641805 hasConcept C166342909 @default.
- W4310641805 hasConcept C181199279 @default.
- W4310641805 hasConcept C185592680 @default.
- W4310641805 hasConcept C204628709 @default.
- W4310641805 hasConcept C2776376580 @default.
- W4310641805 hasConcept C2780283098 @default.
- W4310641805 hasConcept C501734568 @default.
- W4310641805 hasConcept C55493867 @default.
- W4310641805 hasConcept C71240020 @default.
- W4310641805 hasConceptScore W4310641805C104317684 @default.
- W4310641805 hasConceptScore W4310641805C161019410 @default.
- W4310641805 hasConceptScore W4310641805C16318435 @default.
- W4310641805 hasConceptScore W4310641805C166342909 @default.
- W4310641805 hasConceptScore W4310641805C181199279 @default.
- W4310641805 hasConceptScore W4310641805C185592680 @default.