FRINK Linked Data Fragments server

Matches in SemOpenAlex for { <https://semopenalex.org/work/W3034196410> ?p ?o ?g. }

• W3034196410 endingPage "76" @default.
• W3034196410 startingPage "67" @default.
• W3034196410 abstract "ADP-ribosylation is a post-translational modification involved in the regulation of many vital cellular processes. This posttranslational modification is carried out by ADP-ribosyltransferases converting β-NAD+ into nicotinamide and a protein-linked ADP-ribosyl group or a chain of PAR. The reverse reaction, release of ADP-ribose from the acceptor molecule, is catalyzed by ADP-ribosylhydrolases. Several hydrolases contain a macrodomain fold, and activities of human macrodomain protein modules vary from reading or erasing mono- and poly-ADP-ribosylation. Macrodomains have been linked to diseases such as cancer, making them potential drug targets. Discovery of inhibitors requires robust biochemical tools mostly lacking for hydrolases, and here we describe an inhibitor screening assay against mono-ADP-ribosylhydrolyzing enzymes. The activity-based assay uses an α-NAD+, anomer of β-NAD+, which is accepted as a substrate by MacroD1, MacroD2, and ARH3 due to its resemblance to the protein-linked ADP-ribose. The amount of α-NAD+ present after hydrolysis is measured by chemically converting it on a microtiter plate to a fluorescent compound. We optimized the assay for MacroD2 and performed a proof-of-concept compound screening. Three compounds were identified as screening hits with micromolar potency. However, further characterization of the compounds identified them as protein destabilizers, excluding further follow-up studies. Validation and screening demonstrated the usability of the in vitro assay for MacroD2, and we also demonstrate the applicability of the assay as a tool for other human ADP-ribosylhydrolases." @default.
• W3034196410 created "2020-06-19" @default.
• W3034196410 creator A5010330290 @default.
• W3034196410 creator A5010379244 @default.
• W3034196410 creator A5025512055 @default.
• W3034196410 creator A5062886298 @default.
• W3034196410 creator A5089344585 @default.
• W3034196410 date "2021-01-01" @default.
• W3034196410 modified "2023-10-06" @default.
• W3034196410 title "Activity-Based Screening Assay for Mono-ADP-Ribosylhydrolases" @default.
• W3034196410 cites W1965112152 @default.
• W3034196410 cites W1970995808 @default.
• W3034196410 cites W1971806261 @default.
• W3034196410 cites W1991001144 @default.
• W3034196410 cites W1996995837 @default.
• W3034196410 cites W2018402225 @default.
• W3034196410 cites W2023015070 @default.
• W3034196410 cites W2044531033 @default.
• W3034196410 cites W2044565056 @default.
• W3034196410 cites W2061712281 @default.
• W3034196410 cites W2065867569 @default.
• W3034196410 cites W2065915163 @default.
• W3034196410 cites W2068235622 @default.
• W3034196410 cites W2072493619 @default.
• W3034196410 cites W2077775580 @default.
• W3034196410 cites W2110712267 @default.
• W3034196410 cites W2217204947 @default.
• W3034196410 cites W2321071954 @default.
• W3034196410 cites W2334014494 @default.
• W3034196410 cites W2529159010 @default.
• W3034196410 cites W2588135595 @default.
• W3034196410 cites W2750229462 @default.
• W3034196410 cites W2760891778 @default.
• W3034196410 cites W2761766456 @default.
• W3034196410 cites W2766896180 @default.
• W3034196410 cites W2783703589 @default.
• W3034196410 cites W2793726980 @default.
• W3034196410 cites W2810241938 @default.
• W3034196410 cites W2884338874 @default.
• W3034196410 cites W2891031128 @default.
• W3034196410 cites W2896411544 @default.
• W3034196410 cites W2949222247 @default.
• W3034196410 cites W2979537519 @default.
• W3034196410 cites W2994666581 @default.
• W3034196410 doi "https://doi.org/10.1177/2472555220928911" @default.
• W3034196410 hasPubMedId "https://pubmed.ncbi.nlm.nih.gov/32527186" @default.
• W3034196410 hasPublicationYear "2021" @default.
• W3034196410 type Work @default.
• W3034196410 sameAs 3034196410 @default.
• W3034196410 citedByCount "11" @default.
• W3034196410 countsByYear W30341964102020 @default.
• W3034196410 countsByYear W30341964102021 @default.
• W3034196410 countsByYear W30341964102022 @default.
• W3034196410 countsByYear W30341964102023 @default.
• W3034196410 crossrefType "journal-article" @default.
• W3034196410 hasAuthorship W3034196410A5010330290 @default.
• W3034196410 hasAuthorship W3034196410A5010379244 @default.
• W3034196410 hasAuthorship W3034196410A5025512055 @default.
• W3034196410 hasAuthorship W3034196410A5062886298 @default.
• W3034196410 hasAuthorship W3034196410A5089344585 @default.
• W3034196410 hasBestOaLocation W30341964101 @default.
• W3034196410 hasConcept C161624437 @default.
• W3034196410 hasConcept C181199279 @default.
• W3034196410 hasConcept C185592680 @default.
• W3034196410 hasConcept C202751555 @default.
• W3034196410 hasConcept C2779728014 @default.
• W3034196410 hasConcept C55493867 @default.
• W3034196410 hasConcept C74187038 @default.
• W3034196410 hasConcept C75520062 @default.
• W3034196410 hasConcept C86803240 @default.
• W3034196410 hasConceptScore W3034196410C161624437 @default.
• W3034196410 hasConceptScore W3034196410C181199279 @default.
• W3034196410 hasConceptScore W3034196410C185592680 @default.
• W3034196410 hasConceptScore W3034196410C202751555 @default.
• W3034196410 hasConceptScore W3034196410C2779728014 @default.
• W3034196410 hasConceptScore W3034196410C55493867 @default.
• W3034196410 hasConceptScore W3034196410C74187038 @default.
• W3034196410 hasConceptScore W3034196410C75520062 @default.
• W3034196410 hasConceptScore W3034196410C86803240 @default.
• W3034196410 hasFunder F4320323760 @default.
• W3034196410 hasIssue "1" @default.
• W3034196410 hasLocation W30341964101 @default.
• W3034196410 hasLocation W30341964102 @default.
• W3034196410 hasOpenAccess W3034196410 @default.
• W3034196410 hasPrimaryLocation W30341964101 @default.
• W3034196410 hasRelatedWork W1625907927 @default.
• W3034196410 hasRelatedWork W1998484294 @default.
• W3034196410 hasRelatedWork W2035129968 @default.
• W3034196410 hasRelatedWork W2093376715 @default.
• W3034196410 hasRelatedWork W2100495714 @default.
• W3034196410 hasRelatedWork W2147182901 @default.
• W3034196410 hasRelatedWork W2158094397 @default.
• W3034196410 hasRelatedWork W2393553660 @default.
• W3034196410 hasRelatedWork W4230542815 @default.
• W3034196410 hasRelatedWork W4254900740 @default.
• W3034196410 hasVolume "26" @default.
• W3034196410 isParatext "false" @default.
• W3034196410 isRetracted "false" @default.

• next