FRINK Linked Data Fragments server

Matches in SemOpenAlex for { <https://semopenalex.org/work/W2122938153> ?p ?o ?g. }

• W2122938153 endingPage "1396" @default.
• W2122938153 startingPage "1386" @default.
• W2122938153 abstract "Platelet-activating factor (PAF) is a potent pro-inflammatory phospholipid mediator. In response to extracellular stimuli, PAF is rapidly biosynthesized by lyso-PAF acetyltransferase (lyso-PAFAT). Previously, we identified two types of lyso-PAFATs: lysophosphatidylcholine acyltransferase (LPCAT)1, mostly expressed in the lungs where it produces PAF and dipalmitoyl-phosphatidylcholine essential for respiration, and LPCAT2, which biosynthesizes PAF and phosphatidylcholine (PC) in the inflammatory cells. Under inflammatory conditions, LPCAT2, but not LPCAT1, is activated and upregulated to produce PAF. Thus, it is important to develop inhibitors specific for LPCAT2 in order to ameliorate PAF-related inflammatory diseases. Here, we report the first identification of LPCAT2-specific inhibitors, N-phenylmaleimide derivatives, selected from a 174,000-compound library using fluorescence-based high-throughput screening followed by the evaluation of the effects on LPCAT1 and LPCAT2 activities, cell viability, and cellular PAF production. Selected compounds competed with acetyl-CoA for the inhibition of LPCAT2 lyso-PAFAT activity and suppressed PAF biosynthesis in mouse peritoneal macrophages stimulated with a calcium ionophore. These compounds had low inhibitory effects on LPCAT1 activity, indicating that adverse effects on respiratory functions may be avoided. The identified compounds and their derivatives will contribute to the development of novel drugs for PAF-related diseases and facilitate the analysis of LPCAT2 functions in phospholipid metabolism in vivo." @default.
• W2122938153 created "2016-06-24" @default.
• W2122938153 creator A5008934626 @default.
• W2122938153 creator A5025976309 @default.
• W2122938153 creator A5028209311 @default.
• W2122938153 creator A5033586633 @default.
• W2122938153 creator A5035816336 @default.
• W2122938153 creator A5035830409 @default.
• W2122938153 creator A5036596658 @default.
• W2122938153 creator A5044772373 @default.
• W2122938153 creator A5057803965 @default.
• W2122938153 creator A5062413427 @default.
• W2122938153 creator A5071627563 @default.
• W2122938153 date "2014-07-01" @default.
• W2122938153 modified "2023-10-07" @default.
• W2122938153 title "Selective inhibitors of a PAF biosynthetic enzyme lysophosphatidylcholine acyltransferase 2" @default.
• W2122938153 cites W1848597799 @default.
• W2122938153 cites W1942790970 @default.
• W2122938153 cites W1954660491 @default.
• W2122938153 cites W1963128175 @default.
• W2122938153 cites W1967968986 @default.
• W2122938153 cites W1973520510 @default.
• W2122938153 cites W1977911448 @default.
• W2122938153 cites W1978371195 @default.
• W2122938153 cites W1982268890 @default.
• W2122938153 cites W1987932370 @default.
• W2122938153 cites W1997232229 @default.
• W2122938153 cites W2023518167 @default.
• W2122938153 cites W2042815880 @default.
• W2122938153 cites W2049271632 @default.
• W2122938153 cites W2055769271 @default.
• W2122938153 cites W2058786689 @default.
• W2122938153 cites W2066098482 @default.
• W2122938153 cites W2067266295 @default.
• W2122938153 cites W2073084705 @default.
• W2122938153 cites W2075906980 @default.
• W2122938153 cites W2076822925 @default.
• W2122938153 cites W2077369999 @default.
• W2122938153 cites W2079005197 @default.
• W2122938153 cites W2089077776 @default.
• W2122938153 cites W2091509296 @default.
• W2122938153 cites W2094908622 @default.
• W2122938153 cites W2099607826 @default.
• W2122938153 cites W2109850562 @default.
• W2122938153 cites W2120276871 @default.
• W2122938153 cites W2146892797 @default.
• W2122938153 cites W2158572777 @default.
• W2122938153 cites W2168600251 @default.
• W2122938153 cites W2300552860 @default.
• W2122938153 cites W3140086325 @default.
• W2122938153 cites W3192099825 @default.
• W2122938153 doi "https://doi.org/10.1194/jlr.m049205" @default.
• W2122938153 hasPubMedCentralId "https://www.ncbi.nlm.nih.gov/pmc/articles/4076079" @default.
• W2122938153 hasPubMedId "https://pubmed.ncbi.nlm.nih.gov/24850807" @default.
• W2122938153 hasPublicationYear "2014" @default.
• W2122938153 type Work @default.
• W2122938153 sameAs 2122938153 @default.
• W2122938153 citedByCount "21" @default.
• W2122938153 countsByYear W21229381532014 @default.
• W2122938153 countsByYear W21229381532015 @default.
• W2122938153 countsByYear W21229381532017 @default.
• W2122938153 countsByYear W21229381532018 @default.
• W2122938153 countsByYear W21229381532019 @default.
• W2122938153 countsByYear W21229381532020 @default.
• W2122938153 countsByYear W21229381532021 @default.
• W2122938153 countsByYear W21229381532022 @default.
• W2122938153 crossrefType "journal-article" @default.
• W2122938153 hasAuthorship W2122938153A5008934626 @default.
• W2122938153 hasAuthorship W2122938153A5025976309 @default.
• W2122938153 hasAuthorship W2122938153A5028209311 @default.
• W2122938153 hasAuthorship W2122938153A5033586633 @default.
• W2122938153 hasAuthorship W2122938153A5035816336 @default.
• W2122938153 hasAuthorship W2122938153A5035830409 @default.
• W2122938153 hasAuthorship W2122938153A5036596658 @default.
• W2122938153 hasAuthorship W2122938153A5044772373 @default.
• W2122938153 hasAuthorship W2122938153A5057803965 @default.
• W2122938153 hasAuthorship W2122938153A5062413427 @default.
• W2122938153 hasAuthorship W2122938153A5071627563 @default.
• W2122938153 hasBestOaLocation W21229381531 @default.
• W2122938153 hasConcept C104317684 @default.
• W2122938153 hasConcept C119157956 @default.
• W2122938153 hasConcept C181199279 @default.
• W2122938153 hasConcept C185592680 @default.
• W2122938153 hasConcept C203014093 @default.
• W2122938153 hasConcept C2775970874 @default.
• W2122938153 hasConcept C2776330855 @default.
• W2122938153 hasConcept C2778596009 @default.
• W2122938153 hasConcept C2778918659 @default.
• W2122938153 hasConcept C2779020240 @default.
• W2122938153 hasConcept C2779649592 @default.
• W2122938153 hasConcept C41625074 @default.
• W2122938153 hasConcept C55493867 @default.
• W2122938153 hasConcept C86803240 @default.
• W2122938153 hasConcept C98274493 @default.
• W2122938153 hasConceptScore W2122938153C104317684 @default.
• W2122938153 hasConceptScore W2122938153C119157956 @default.
• W2122938153 hasConceptScore W2122938153C181199279 @default.
• W2122938153 hasConceptScore W2122938153C185592680 @default.

• next