Matches in SemOpenAlex for { <https://semopenalex.org/work/W1986018051> ?p ?o ?g. }
Showing items 1 to 100 of
100
with 100 items per page.
- W1986018051 endingPage "753" @default.
- W1986018051 startingPage "745" @default.
- W1986018051 abstract "We hypothesized that aryl acetate- and aryl carboxylate-containing drugs would inhibit human phenol sulfotransferase (SULT1A1), and that selectivity would depend upon the interaction of the aryl portion of the molecule with the sulfotransferase acceptor binding site. This hypothesis was based on results with the rat orthologue showing that oxidation of phenolic substrates to carboxylate derivatives resulted in competitive inhibition of rat phenol sulfotransferase. We chose nine structurally representative non-steroidal anti-inflammatory agents and determined their inhibitory potency and selectivity toward SULT1A1 and expressed human estrogen sulfotransferase (SULT1E1). The results show that the tested agents reversibly inhibit SULT1A1 activity with IC50 ranging from 0.1 μM to 3800 μM. These agents also inhibited SULT1E1 (IC50 = 6 μM to 9000 μM). The agents were clearly isoform selective, with IC50 ratios (1E1/1A1) ranging from 0.01 to 200. Nimesulide, meclofenamate, and piroxicam were more selective towards SULT1A1 inhibition, while sulindac and ibuprofen were more selective towards SULT1E1 inhibition. Sulfotransferase inhibition was maintained after substituting the carboxylate with enolate (nimesulide) or methylsulfonamide (piroxicam). Kinetic studies determined the type of inhibition of SULT1A1 for three agents (meclofenamate, nimesulide, aspirin) to be non-competitive or partial noncompetitive versus both substrate (p-nitrophenol) and cofactor (PAPS). This inhibition mechanism indicates that meclofenamate, nimesulide and aspirin bind near enough to the substrate binding site to prevent catalysis but not affect dissociation of the substrate-enzyme complex. The inhibition of SULT1A1 by meclofenamate, nimesulide, salicylate and aspirin may be clinically relevant based on ratio of inhibition constant to predicted in vivo inhibitor concentration ([I]/IC50 > 1). Keywords: Human SULT1A1, human SULT1E1, human liver cytosol, non-steroidal anti-inflammatory, inhibition of sulfonation, sulfotransferase" @default.
- W1986018051 created "2016-06-24" @default.
- W1986018051 creator A5043979826 @default.
- W1986018051 creator A5055235091 @default.
- W1986018051 creator A5078119764 @default.
- W1986018051 date "2006-10-01" @default.
- W1986018051 modified "2023-10-16" @default.
- W1986018051 title "Inhibition of Human Phenol and Estrogen Sulfotransferase by Certain Non-Steroidal Anti-Inflammatory Agents" @default.
- W1986018051 cites W172537485 @default.
- W1986018051 cites W1797210820 @default.
- W1986018051 cites W1968379731 @default.
- W1986018051 cites W1982779500 @default.
- W1986018051 cites W2036333800 @default.
- W1986018051 cites W2042984106 @default.
- W1986018051 cites W2048366562 @default.
- W1986018051 cites W2066749355 @default.
- W1986018051 cites W2072010935 @default.
- W1986018051 cites W2083703737 @default.
- W1986018051 cites W2087498613 @default.
- W1986018051 cites W2088904918 @default.
- W1986018051 cites W2130145312 @default.
- W1986018051 cites W2130266468 @default.
- W1986018051 cites W2140155372 @default.
- W1986018051 cites W2154301892 @default.
- W1986018051 cites W2156123044 @default.
- W1986018051 cites W2401123559 @default.
- W1986018051 cites W2430311521 @default.
- W1986018051 doi "https://doi.org/10.2174/138920006778520615" @default.
- W1986018051 hasPubMedCentralId "https://www.ncbi.nlm.nih.gov/pmc/articles/2105742" @default.
- W1986018051 hasPubMedId "https://pubmed.ncbi.nlm.nih.gov/17073578" @default.
- W1986018051 hasPublicationYear "2006" @default.
- W1986018051 type Work @default.
- W1986018051 sameAs 1986018051 @default.
- W1986018051 citedByCount "30" @default.
- W1986018051 countsByYear W19860180512012 @default.
- W1986018051 countsByYear W19860180512013 @default.
- W1986018051 countsByYear W19860180512014 @default.
- W1986018051 countsByYear W19860180512015 @default.
- W1986018051 countsByYear W19860180512016 @default.
- W1986018051 countsByYear W19860180512017 @default.
- W1986018051 countsByYear W19860180512018 @default.
- W1986018051 countsByYear W19860180512021 @default.
- W1986018051 countsByYear W19860180512022 @default.
- W1986018051 crossrefType "journal-article" @default.
- W1986018051 hasAuthorship W1986018051A5043979826 @default.
- W1986018051 hasAuthorship W1986018051A5055235091 @default.
- W1986018051 hasAuthorship W1986018051A5078119764 @default.
- W1986018051 hasBestOaLocation W19860180512 @default.
- W1986018051 hasConcept C142724271 @default.
- W1986018051 hasConcept C150757390 @default.
- W1986018051 hasConcept C155138218 @default.
- W1986018051 hasConcept C181199279 @default.
- W1986018051 hasConcept C185592680 @default.
- W1986018051 hasConcept C204787440 @default.
- W1986018051 hasConcept C2775904581 @default.
- W1986018051 hasConcept C2777570176 @default.
- W1986018051 hasConcept C2778139025 @default.
- W1986018051 hasConcept C2779475777 @default.
- W1986018051 hasConcept C55493867 @default.
- W1986018051 hasConcept C71240020 @default.
- W1986018051 hasConcept C71924100 @default.
- W1986018051 hasConcept C98274493 @default.
- W1986018051 hasConceptScore W1986018051C142724271 @default.
- W1986018051 hasConceptScore W1986018051C150757390 @default.
- W1986018051 hasConceptScore W1986018051C155138218 @default.
- W1986018051 hasConceptScore W1986018051C181199279 @default.
- W1986018051 hasConceptScore W1986018051C185592680 @default.
- W1986018051 hasConceptScore W1986018051C204787440 @default.
- W1986018051 hasConceptScore W1986018051C2775904581 @default.
- W1986018051 hasConceptScore W1986018051C2777570176 @default.
- W1986018051 hasConceptScore W1986018051C2778139025 @default.
- W1986018051 hasConceptScore W1986018051C2779475777 @default.
- W1986018051 hasConceptScore W1986018051C55493867 @default.
- W1986018051 hasConceptScore W1986018051C71240020 @default.
- W1986018051 hasConceptScore W1986018051C71924100 @default.
- W1986018051 hasConceptScore W1986018051C98274493 @default.
- W1986018051 hasIssue "7" @default.
- W1986018051 hasLocation W19860180511 @default.
- W1986018051 hasLocation W19860180512 @default.
- W1986018051 hasLocation W19860180513 @default.
- W1986018051 hasLocation W19860180514 @default.
- W1986018051 hasOpenAccess W1986018051 @default.
- W1986018051 hasPrimaryLocation W19860180511 @default.
- W1986018051 hasRelatedWork W1970659991 @default.
- W1986018051 hasRelatedWork W1975340112 @default.
- W1986018051 hasRelatedWork W1986018051 @default.
- W1986018051 hasRelatedWork W2000259043 @default.
- W1986018051 hasRelatedWork W2063679949 @default.
- W1986018051 hasRelatedWork W2121624034 @default.
- W1986018051 hasRelatedWork W2142319763 @default.
- W1986018051 hasRelatedWork W2362781159 @default.
- W1986018051 hasRelatedWork W2886656117 @default.
- W1986018051 hasRelatedWork W4210689950 @default.
- W1986018051 hasVolume "7" @default.
- W1986018051 isParatext "false" @default.
- W1986018051 isRetracted "false" @default.
- W1986018051 magId "1986018051" @default.
- W1986018051 workType "article" @default.