FRINK Linked Data Fragments server

Matches in SemOpenAlex for { <https://semopenalex.org/work/W2783997690> ?p ?o ?g. }

• W2783997690 endingPage "e2003887" @default.
• W2783997690 startingPage "e2003887" @default.
• W2783997690 abstract "Urease as a potential target of antimicrobial drugs has received considerable attention given its versatile roles in microbial infection. Development of effective urease inhibitors, however, is a significant challenge due to the deeply buried active site and highly specific substrate of a bacterial urease. Conventionally, urease inhibitors are designed by either targeting the active site or mimicking substrate of urease, which is not efficient. Up to now, only one effective inhibitor-acetohydroxamic acid (AHA)-is clinically available, but it has adverse side effects. Herein, we demonstrate that a clinically used drug, colloidal bismuth subcitrate, utilizes an unusual way to inhibit urease activity, i.e., disruption of urease maturation process via functional perturbation of a metallochaperone, UreG. Similar phenomena were also observed in various pathogenic bacteria, suggesting that UreG may serve as a general target for design of new types of urease inhibitors. Using Helicobacter pylori UreG as a showcase, by virtual screening combined with experimental validation, we show that two compounds targeting UreG also efficiently inhibited urease activity with inhibitory concentration (IC)50 values of micromolar level, resulting in attenuated virulence of the pathogen. We further demonstrate the efficacy of the compounds in a mammalian cell infection model. This study opens up a new opportunity for the design of more effective urease inhibitors and clearly indicates that metallochaperones involved in the maturation of important microbial metalloenzymes serve as new targets for devising a new type of antimicrobial drugs." @default.
• W2783997690 created "2018-01-26" @default.
• W2783997690 creator A5001800281 @default.
• W2783997690 creator A5017803324 @default.
• W2783997690 creator A5020865835 @default.
• W2783997690 creator A5021738077 @default.
• W2783997690 creator A5044554947 @default.
• W2783997690 creator A5051082404 @default.
• W2783997690 creator A5080624294 @default.
• W2783997690 creator A5086445887 @default.
• W2783997690 date "2018-01-10" @default.
• W2783997690 modified "2023-10-15" @default.
• W2783997690 title "Metallochaperone UreG serves as a new target for design of urease inhibitor: A novel strategy for development of antimicrobials" @default.
• W2783997690 cites W1912217738 @default.
• W2783997690 cites W1933287277 @default.
• W2783997690 cites W1965182355 @default.
• W2783997690 cites W1967539008 @default.
• W2783997690 cites W1969451473 @default.
• W2783997690 cites W1970372029 @default.
• W2783997690 cites W1972055505 @default.
• W2783997690 cites W1975572214 @default.
• W2783997690 cites W1980421436 @default.
• W2783997690 cites W1980447876 @default.
• W2783997690 cites W1984850609 @default.
• W2783997690 cites W1985953075 @default.
• W2783997690 cites W1989874926 @default.
• W2783997690 cites W2000312207 @default.
• W2783997690 cites W2002862262 @default.
• W2783997690 cites W2004457911 @default.
• W2783997690 cites W2004519217 @default.
• W2783997690 cites W2007731336 @default.
• W2783997690 cites W2015304573 @default.
• W2783997690 cites W2029149649 @default.
• W2783997690 cites W2031240692 @default.
• W2783997690 cites W2058170418 @default.
• W2783997690 cites W2059009998 @default.
• W2783997690 cites W2059114873 @default.
• W2783997690 cites W2060583246 @default.
• W2783997690 cites W2061117754 @default.
• W2783997690 cites W2064597227 @default.
• W2783997690 cites W2065389516 @default.
• W2783997690 cites W2071816962 @default.
• W2783997690 cites W2075345553 @default.
• W2783997690 cites W2076123206 @default.
• W2783997690 cites W2095041765 @default.
• W2783997690 cites W2096266405 @default.
• W2783997690 cites W2105668062 @default.
• W2783997690 cites W2108317022 @default.
• W2783997690 cites W2109587986 @default.
• W2783997690 cites W2109987434 @default.
• W2783997690 cites W2114521758 @default.
• W2783997690 cites W2121731147 @default.
• W2783997690 cites W2122002065 @default.
• W2783997690 cites W2133479466 @default.
• W2783997690 cites W2134967712 @default.
• W2783997690 cites W2147512361 @default.
• W2783997690 cites W2158123709 @default.
• W2783997690 cites W2193666963 @default.
• W2783997690 cites W2204695023 @default.
• W2783997690 cites W2263960908 @default.
• W2783997690 cites W2314723537 @default.
• W2783997690 cites W2337653620 @default.
• W2783997690 cites W2606975737 @default.
• W2783997690 cites W2916534270 @default.
• W2783997690 cites W4254246059 @default.
• W2783997690 doi "https://doi.org/10.1371/journal.pbio.2003887" @default.
• W2783997690 hasPubMedCentralId "https://www.ncbi.nlm.nih.gov/pmc/articles/5779714" @default.
• W2783997690 hasPubMedId "https://pubmed.ncbi.nlm.nih.gov/29320492" @default.
• W2783997690 hasPublicationYear "2018" @default.
• W2783997690 type Work @default.
• W2783997690 sameAs 2783997690 @default.
• W2783997690 citedByCount "30" @default.
• W2783997690 countsByYear W27839976902018 @default.
• W2783997690 countsByYear W27839976902019 @default.
• W2783997690 countsByYear W27839976902020 @default.
• W2783997690 countsByYear W27839976902021 @default.
• W2783997690 countsByYear W27839976902022 @default.
• W2783997690 countsByYear W27839976902023 @default.
• W2783997690 crossrefType "journal-article" @default.
• W2783997690 hasAuthorship W2783997690A5001800281 @default.
• W2783997690 hasAuthorship W2783997690A5017803324 @default.
• W2783997690 hasAuthorship W2783997690A5020865835 @default.
• W2783997690 hasAuthorship W2783997690A5021738077 @default.
• W2783997690 hasAuthorship W2783997690A5044554947 @default.
• W2783997690 hasAuthorship W2783997690A5051082404 @default.
• W2783997690 hasAuthorship W2783997690A5080624294 @default.
• W2783997690 hasAuthorship W2783997690A5086445887 @default.
• W2783997690 hasBestOaLocation W27839976901 @default.
• W2783997690 hasConcept C181199279 @default.
• W2783997690 hasConcept C185592680 @default.
• W2783997690 hasConcept C2779521917 @default.
• W2783997690 hasConcept C2781421780 @default.
• W2783997690 hasConcept C4937899 @default.
• W2783997690 hasConcept C55493867 @default.
• W2783997690 hasConcept C86803240 @default.
• W2783997690 hasConcept C89423630 @default.
• W2783997690 hasConceptScore W2783997690C181199279 @default.
• W2783997690 hasConceptScore W2783997690C185592680 @default.

• next