Matches in SemOpenAlex for { <https://semopenalex.org/work/W3176604443> ?p ?o ?g. }
- W3176604443 endingPage "1953" @default.
- W3176604443 startingPage "1941" @default.
- W3176604443 abstract "Both the soil bacterium Chromobacterium vaccinii and the bacterial endosymbiont Candidatus Burkholderia crenata of the plant Ardisia crenata are producers of FR900359 (FR). This cyclic depsipeptide is a potent and selective Gq protein inhibitor used extensively to investigate the intracellular signaling of G protein coupled receptors (GPCRs). In this study, the metabolomes of both FR producers were investigated and compared using feature-based molecular networking (FBMN). As a result, 30 previously unknown FR derivatives were identified, one-third being unique to C. vaccinii. Guided by MS, a novel FR derivative, FR-6 (compound 1), was isolated, and its structure unambiguously established. In a whole-cell biosensing assay based on detection of dynamic mass redistribution (DMR) as readout for Gq inhibition, FR-6 suppressed Gq signaling with micromolar potency (pIC50 = 5.56). This functional activity was confirmed in radioligand binding assays (pKi = 7.50). This work demonstrates the power of molecular networking, guiding the way to a novel Gq-inhibiting FR derivative and underlining the potency of FR as a Gq inhibitor." @default.
- W3176604443 created "2021-07-05" @default.
- W3176604443 creator A5010166957 @default.
- W3176604443 creator A5017260514 @default.
- W3176604443 creator A5027498283 @default.
- W3176604443 creator A5027819899 @default.
- W3176604443 creator A5029710086 @default.
- W3176604443 creator A5051782577 @default.
- W3176604443 creator A5054216760 @default.
- W3176604443 creator A5058056833 @default.
- W3176604443 creator A5061959920 @default.
- W3176604443 creator A5063472068 @default.
- W3176604443 creator A5071041494 @default.
- W3176604443 creator A5077768594 @default.
- W3176604443 creator A5078003125 @default.
- W3176604443 creator A5078965540 @default.
- W3176604443 date "2021-07-01" @default.
- W3176604443 modified "2023-10-15" @default.
- W3176604443 title "Feature-Based Molecular Networking for the Targeted Identification of G<sub>q</sub>-Inhibiting FR900359 Derivatives" @default.
- W3176604443 cites W1495926848 @default.
- W3176604443 cites W1594539819 @default.
- W3176604443 cites W1973650867 @default.
- W3176604443 cites W1989299822 @default.
- W3176604443 cites W2004503265 @default.
- W3176604443 cites W2004871593 @default.
- W3176604443 cites W2013428424 @default.
- W3176604443 cites W2017316435 @default.
- W3176604443 cites W2033334651 @default.
- W3176604443 cites W2065386792 @default.
- W3176604443 cites W2082633436 @default.
- W3176604443 cites W2105668062 @default.
- W3176604443 cites W2109967142 @default.
- W3176604443 cites W2154222508 @default.
- W3176604443 cites W2170393885 @default.
- W3176604443 cites W2189959630 @default.
- W3176604443 cites W2259804540 @default.
- W3176604443 cites W2489364496 @default.
- W3176604443 cites W2499293014 @default.
- W3176604443 cites W2504691963 @default.
- W3176604443 cites W2517883571 @default.
- W3176604443 cites W2581766148 @default.
- W3176604443 cites W2582032120 @default.
- W3176604443 cites W2707623555 @default.
- W3176604443 cites W2740856177 @default.
- W3176604443 cites W2753967201 @default.
- W3176604443 cites W2781264868 @default.
- W3176604443 cites W2806430985 @default.
- W3176604443 cites W2810596438 @default.
- W3176604443 cites W2912179268 @default.
- W3176604443 cites W2922555277 @default.
- W3176604443 cites W2947129631 @default.
- W3176604443 cites W2953020760 @default.
- W3176604443 cites W2998575629 @default.
- W3176604443 cites W3009596360 @default.
- W3176604443 cites W3038239843 @default.
- W3176604443 cites W3080789666 @default.
- W3176604443 cites W3119640666 @default.
- W3176604443 cites W3123030036 @default.
- W3176604443 doi "https://doi.org/10.1021/acs.jnatprod.1c00194" @default.
- W3176604443 hasPubMedId "https://pubmed.ncbi.nlm.nih.gov/34197116" @default.
- W3176604443 hasPublicationYear "2021" @default.
- W3176604443 type Work @default.
- W3176604443 sameAs 3176604443 @default.
- W3176604443 citedByCount "6" @default.
- W3176604443 countsByYear W31766044432021 @default.
- W3176604443 countsByYear W31766044432022 @default.
- W3176604443 countsByYear W31766044432023 @default.
- W3176604443 crossrefType "journal-article" @default.
- W3176604443 hasAuthorship W3176604443A5010166957 @default.
- W3176604443 hasAuthorship W3176604443A5017260514 @default.
- W3176604443 hasAuthorship W3176604443A5027498283 @default.
- W3176604443 hasAuthorship W3176604443A5027819899 @default.
- W3176604443 hasAuthorship W3176604443A5029710086 @default.
- W3176604443 hasAuthorship W3176604443A5051782577 @default.
- W3176604443 hasAuthorship W3176604443A5054216760 @default.
- W3176604443 hasAuthorship W3176604443A5058056833 @default.
- W3176604443 hasAuthorship W3176604443A5061959920 @default.
- W3176604443 hasAuthorship W3176604443A5063472068 @default.
- W3176604443 hasAuthorship W3176604443A5071041494 @default.
- W3176604443 hasAuthorship W3176604443A5077768594 @default.
- W3176604443 hasAuthorship W3176604443A5078003125 @default.
- W3176604443 hasAuthorship W3176604443A5078965540 @default.
- W3176604443 hasConcept C185592680 @default.
- W3176604443 hasConcept C55493867 @default.
- W3176604443 hasConcept C71240020 @default.
- W3176604443 hasConcept C86803240 @default.
- W3176604443 hasConceptScore W3176604443C185592680 @default.
- W3176604443 hasConceptScore W3176604443C55493867 @default.
- W3176604443 hasConceptScore W3176604443C71240020 @default.
- W3176604443 hasConceptScore W3176604443C86803240 @default.
- W3176604443 hasFunder F4320309954 @default.
- W3176604443 hasFunder F4320320879 @default.
- W3176604443 hasIssue "7" @default.
- W3176604443 hasLocation W31766044431 @default.
- W3176604443 hasLocation W31766044432 @default.
- W3176604443 hasOpenAccess W3176604443 @default.
- W3176604443 hasPrimaryLocation W31766044431 @default.
- W3176604443 hasRelatedWork W1531601525 @default.