FRINK Linked Data Fragments server

Matches in SemOpenAlex for { <https://semopenalex.org/work/W4200219833> ?p ?o ?g. }

• W4200219833 endingPage "132278" @default.
• W4200219833 startingPage "132278" @default.
• W4200219833 abstract "Latent tuberculosis infection is caused by Mycobacterium tuberculosis (Mtb) persistence and poses a significant challenge to the eradication of tuberculosis. The detection of Mtb DevR/DosR dormancy regulon expression in clinical specimens has provided evidence for the existence of persistent/dormant tubercle bacilli in vivo. Targeting of DevR is expected to eliminate these persisters that are tolerant to anti-tubercular drugs. The presence of redundant pathways of DevR activation in Mtb necessitates targeting DevR, and not its cognate sensor kinases, DevS and DosT. Drug discovery programs are heavily dependent on inhibitor screening assays. Here, we report a high throughput screening assay in Mtb termed ReFPA (Real Time Fluorescence Plate Assay) to identify inhibitors that specifically target DevR. Using ReFPA, we identified novel thiazolidin-4-one-based inhibitors of DevR, namely N5, N6 and N11, that interfered with the hypoxic viability of Mycobacterium bovis BCG and were non-toxic to HepG2 cells. In silico docking analysis revealed that N5, N6 and N11 bound to a common pocket located in the C-terminal domain of DevR. The interaction of N5, N6 and N11 with DevR was experimentally confirmed using thermal shift assay. These findings demonstrate the identification of a new and promising scaffold to design anti-DevR molecules for intercepting mycobacterial dormancy." @default.
• W4200219833 created "2021-12-31" @default.
• W4200219833 creator A5009383670 @default.
• W4200219833 creator A5015696485 @default.
• W4200219833 creator A5034034338 @default.
• W4200219833 creator A5042223331 @default.
• W4200219833 creator A5052412003 @default.
• W4200219833 creator A5058278938 @default.
• W4200219833 creator A5059245133 @default.
• W4200219833 creator A5063079118 @default.
• W4200219833 date "2022-04-01" @default.
• W4200219833 modified "2023-09-25" @default.
• W4200219833 title "Novel benzoic thiazolidin-4-one derivatives targeting DevR/DosR dormancy regulator of Mycobacterium tuberculosis" @default.
• W4200219833 cites W1969248605 @default.
• W4200219833 cites W1969787083 @default.
• W4200219833 cites W1971127707 @default.
• W4200219833 cites W1987684543 @default.
• W4200219833 cites W1991371091 @default.
• W4200219833 cites W2014451521 @default.
• W4200219833 cites W2027463615 @default.
• W4200219833 cites W2044212859 @default.
• W4200219833 cites W2052791500 @default.
• W4200219833 cites W2053609853 @default.
• W4200219833 cites W2067828311 @default.
• W4200219833 cites W2080354196 @default.
• W4200219833 cites W2081705993 @default.
• W4200219833 cites W2084171643 @default.
• W4200219833 cites W2120960383 @default.
• W4200219833 cites W2142672833 @default.
• W4200219833 cites W2145072890 @default.
• W4200219833 cites W2159669055 @default.
• W4200219833 cites W2165780813 @default.
• W4200219833 cites W2281605531 @default.
• W4200219833 cites W2289382092 @default.
• W4200219833 cites W2794376461 @default.
• W4200219833 cites W2907865617 @default.
• W4200219833 cites W3004216838 @default.
• W4200219833 cites W3006429145 @default.
• W4200219833 cites W3188597707 @default.
• W4200219833 doi "https://doi.org/10.1016/j.molstruc.2021.132278" @default.
• W4200219833 hasPublicationYear "2022" @default.
• W4200219833 type Work @default.
• W4200219833 citedByCount "2" @default.
• W4200219833 countsByYear W42002198332022 @default.
• W4200219833 crossrefType "journal-article" @default.
• W4200219833 hasAuthorship W4200219833A5009383670 @default.
• W4200219833 hasAuthorship W4200219833A5015696485 @default.
• W4200219833 hasAuthorship W4200219833A5034034338 @default.
• W4200219833 hasAuthorship W4200219833A5042223331 @default.
• W4200219833 hasAuthorship W4200219833A5052412003 @default.
• W4200219833 hasAuthorship W4200219833A5058278938 @default.
• W4200219833 hasAuthorship W4200219833A5059245133 @default.
• W4200219833 hasAuthorship W4200219833A5063079118 @default.
• W4200219833 hasConcept C104317684 @default.
• W4200219833 hasConcept C142724271 @default.
• W4200219833 hasConcept C159110408 @default.
• W4200219833 hasConcept C185592680 @default.
• W4200219833 hasConcept C2775905019 @default.
• W4200219833 hasConcept C2777975735 @default.
• W4200219833 hasConcept C2778497218 @default.
• W4200219833 hasConcept C2781069245 @default.
• W4200219833 hasConcept C41685203 @default.
• W4200219833 hasConcept C51323132 @default.
• W4200219833 hasConcept C55493867 @default.
• W4200219833 hasConcept C62361671 @default.
• W4200219833 hasConcept C6929976 @default.
• W4200219833 hasConcept C70721500 @default.
• W4200219833 hasConcept C71924100 @default.
• W4200219833 hasConcept C86339819 @default.
• W4200219833 hasConcept C86803240 @default.
• W4200219833 hasConceptScore W4200219833C104317684 @default.
• W4200219833 hasConceptScore W4200219833C142724271 @default.
• W4200219833 hasConceptScore W4200219833C159110408 @default.
• W4200219833 hasConceptScore W4200219833C185592680 @default.
• W4200219833 hasConceptScore W4200219833C2775905019 @default.
• W4200219833 hasConceptScore W4200219833C2777975735 @default.
• W4200219833 hasConceptScore W4200219833C2778497218 @default.
• W4200219833 hasConceptScore W4200219833C2781069245 @default.
• W4200219833 hasConceptScore W4200219833C41685203 @default.
• W4200219833 hasConceptScore W4200219833C51323132 @default.
• W4200219833 hasConceptScore W4200219833C55493867 @default.
• W4200219833 hasConceptScore W4200219833C62361671 @default.
• W4200219833 hasConceptScore W4200219833C6929976 @default.
• W4200219833 hasConceptScore W4200219833C70721500 @default.
• W4200219833 hasConceptScore W4200219833C71924100 @default.
• W4200219833 hasConceptScore W4200219833C86339819 @default.
• W4200219833 hasConceptScore W4200219833C86803240 @default.
• W4200219833 hasLocation W42002198331 @default.
• W4200219833 hasOpenAccess W4200219833 @default.
• W4200219833 hasPrimaryLocation W42002198331 @default.
• W4200219833 hasRelatedWork W2056382779 @default.
• W4200219833 hasRelatedWork W2140251613 @default.
• W4200219833 hasRelatedWork W2150743143 @default.
• W4200219833 hasRelatedWork W2168152179 @default.
• W4200219833 hasRelatedWork W2526831331 @default.
• W4200219833 hasRelatedWork W2952264303 @default.
• W4200219833 hasRelatedWork W3089848551 @default.
• W4200219833 hasRelatedWork W3207154492 @default.

• next