FRINK Linked Data Fragments server

Matches in SemOpenAlex for { <https://semopenalex.org/work/W1489667240> ?p ?o ?g. }

• W1489667240 abstract "Giardiasis caused by Giardia intestinalis (syn. G. lamblia, G. duodenalis) is one of the leading causes of diarrheal parasitic diseases worldwide. Although limited drugs to treat giardiasis are available, there are concerns regarding toxicity in some patients and the emerging drug resistance. By data-mining genome sequences, we observed that G. intestinalis is incapable of synthesizing fatty acids (FA) de novo. However, this parasite has five long-chain fatty acyl-CoA synthetases (GiACS1 to GiACS5) to activate FA scavenged from the host. ACS is an essential enzyme because FA need to be activated to form acyl-CoA thioesters before they can enter subsequent metabolism. In the present study, we performed experiments to explore whether some GiACS enzymes could serve as drug targets in Giardia. Based on the high-throughput datasets and protein modeling analyses, we initially studied the GiACS1 and GiACS2, because genes encoding these two enzymes were found to be more consistently expressed in varied parasite life cycle stages and when interacting with host cells based on previously reported transcriptome data. These two proteins were cloned and expressed as recombinant proteins. Biochemical analysis revealed that both had apparent substrate preference toward palmitic acid (C16:0) and myristic acid (C14:0), and allosteric or Michaelis-Menten kinetics on palmitic acid or ATP. The ACS inhibitor triacsin C inhibited the activity of both enzymes (IC50 = 1.56 μM, K i = 0.18 μM for GiACS1, and IC50 = 2.28 μM, K i = 0.23 μM for GiACS2, respectively) and the growth of G. intestinalis in vitro (IC50 = 0.8 μM). As expected from giardial evolutionary characteristics, both GiACSs displayed differences in overall folding structure as compared with their human counterparts. These observations support the notion that some of the GiACS enzymes may be explored as drug targets in this parasite." @default.
• W1489667240 created "2016-06-24" @default.
• W1489667240 creator A5000662999 @default.
• W1489667240 creator A5002628473 @default.
• W1489667240 creator A5027672178 @default.
• W1489667240 creator A5080473175 @default.
• W1489667240 creator A5091567029 @default.
• W1489667240 date "2015-07-22" @default.
• W1489667240 modified "2023-10-10" @default.
• W1489667240 title "Giardia fatty acyl-CoA synthetases as potential drug targets" @default.
• W1489667240 cites W1563007037 @default.
• W1489667240 cites W1819563916 @default.
• W1489667240 cites W1975336675 @default.
• W1489667240 cites W1978570354 @default.
• W1489667240 cites W1978910067 @default.
• W1489667240 cites W1979794194 @default.
• W1489667240 cites W1979824753 @default.
• W1489667240 cites W1982857474 @default.
• W1489667240 cites W1987134040 @default.
• W1489667240 cites W1995629720 @default.
• W1489667240 cites W2001255062 @default.
• W1489667240 cites W2007953509 @default.
• W1489667240 cites W2016185570 @default.
• W1489667240 cites W2021372863 @default.
• W1489667240 cites W2021672507 @default.
• W1489667240 cites W2037312364 @default.
• W1489667240 cites W2043207375 @default.
• W1489667240 cites W2045186739 @default.
• W1489667240 cites W2068680153 @default.
• W1489667240 cites W2071826229 @default.
• W1489667240 cites W2074631079 @default.
• W1489667240 cites W2078905435 @default.
• W1489667240 cites W2084853343 @default.
• W1489667240 cites W2092239717 @default.
• W1489667240 cites W2093440481 @default.
• W1489667240 cites W2099504037 @default.
• W1489667240 cites W2108859352 @default.
• W1489667240 cites W2109277407 @default.
• W1489667240 cites W2111040550 @default.
• W1489667240 cites W2127244533 @default.
• W1489667240 cites W2147043577 @default.
• W1489667240 cites W2155201844 @default.
• W1489667240 cites W2160193305 @default.
• W1489667240 cites W2168676619 @default.
• W1489667240 cites W2169999342 @default.
• W1489667240 cites W2331674272 @default.
• W1489667240 cites W2332348819 @default.
• W1489667240 cites W2338931439 @default.
• W1489667240 cites W2418146721 @default.
• W1489667240 cites W2916778917 @default.
• W1489667240 cites W2917877471 @default.
• W1489667240 cites W4299365787 @default.
• W1489667240 doi "https://doi.org/10.3389/fmicb.2015.00753" @default.
• W1489667240 hasPubMedCentralId "https://www.ncbi.nlm.nih.gov/pmc/articles/4510421" @default.
• W1489667240 hasPubMedId "https://pubmed.ncbi.nlm.nih.gov/26257723" @default.
• W1489667240 hasPublicationYear "2015" @default.
• W1489667240 type Work @default.
• W1489667240 sameAs 1489667240 @default.
• W1489667240 citedByCount "9" @default.
• W1489667240 countsByYear W14896672402016 @default.
• W1489667240 countsByYear W14896672402017 @default.
• W1489667240 countsByYear W14896672402019 @default.
• W1489667240 countsByYear W14896672402020 @default.
• W1489667240 countsByYear W14896672402021 @default.
• W1489667240 countsByYear W14896672402022 @default.
• W1489667240 countsByYear W14896672402023 @default.
• W1489667240 crossrefType "journal-article" @default.
• W1489667240 hasAuthorship W1489667240A5000662999 @default.
• W1489667240 hasAuthorship W1489667240A5002628473 @default.
• W1489667240 hasAuthorship W1489667240A5027672178 @default.
• W1489667240 hasAuthorship W1489667240A5080473175 @default.
• W1489667240 hasAuthorship W1489667240A5091567029 @default.
• W1489667240 hasBestOaLocation W14896672401 @default.
• W1489667240 hasConcept C104317684 @default.
• W1489667240 hasConcept C181199279 @default.
• W1489667240 hasConcept C202751555 @default.
• W1489667240 hasConcept C2777271458 @default.
• W1489667240 hasConcept C2777752497 @default.
• W1489667240 hasConcept C2779936771 @default.
• W1489667240 hasConcept C2780626423 @default.
• W1489667240 hasConcept C543025807 @default.
• W1489667240 hasConcept C55493867 @default.
• W1489667240 hasConcept C86803240 @default.
• W1489667240 hasConcept C89423630 @default.
• W1489667240 hasConceptScore W1489667240C104317684 @default.
• W1489667240 hasConceptScore W1489667240C181199279 @default.
• W1489667240 hasConceptScore W1489667240C202751555 @default.
• W1489667240 hasConceptScore W1489667240C2777271458 @default.
• W1489667240 hasConceptScore W1489667240C2777752497 @default.
• W1489667240 hasConceptScore W1489667240C2779936771 @default.
• W1489667240 hasConceptScore W1489667240C2780626423 @default.
• W1489667240 hasConceptScore W1489667240C543025807 @default.
• W1489667240 hasConceptScore W1489667240C55493867 @default.
• W1489667240 hasConceptScore W1489667240C86803240 @default.
• W1489667240 hasConceptScore W1489667240C89423630 @default.
• W1489667240 hasLocation W14896672401 @default.
• W1489667240 hasLocation W14896672402 @default.
• W1489667240 hasLocation W14896672403 @default.
• W1489667240 hasLocation W14896672404 @default.
• W1489667240 hasLocation W14896672405 @default.

• next