FRINK Linked Data Fragments server

Matches in SemOpenAlex for { <https://semopenalex.org/work/W2099802056> ?p ?o ?g. }

• W2099802056 endingPage "194" @default.
• W2099802056 startingPage "183" @default.
• W2099802056 abstract "ABSTRACT The in vitro metabolic stability and transport mechanism of TM‐25659, a novel TAZ modulator, was investigated in human hepatocytes and human liver microsomes (HLMs) based on the preferred hepatobiliary elimination in rats. In addition, the in vitro transport mechanism and transporter‐mediated drug–drug interactions were evaluated using oocytes and MDCKII cells overexpressing clinically important drug transporters. After a 1 h incubation in HLMs, 92.9 ± 9.5% and 95.5 ± 11.6% of the initial TM‐25659 remained in the presence of NADPH and UDPGA, respectively. Uptake of TM‐25659 readily accumulated in human hepatocytes at 37 ºC (i.e. 6.7‐fold greater than that at 4 ºC), in which drug transporters such as OATP1B1 and OATP1B3 were involved. TM‐25659 had a significantly greater basal to apical transport rate (5.9‐fold) than apical to basal transport rate in the Caco‐2 cell monolayer, suggesting the involvement of an efflux transport system. Further studies using inhibitors of efflux transporters and overexpressing cells revealed that MRP2 was involved in the transport of TM‐25659. These results, taken together, suggested that TM‐25659 can be actively influxed into hepatocytes and undergo biliary excretion without substantial metabolism. Additionally, TM‐25659 inhibited the transport activities of OATP1B1 and OATP1B3 with IC 50 values of 36.3 and 25.9 μ m , respectively. TM‐25659 (100 μ m ) increased the accumulation of the probe substrate by 160% and 213%, respectively, through the inhibition of efflux function of P‐gp and MRP2. In conclusion, OATP1B1, OATP1B3, P‐gp and MRP2 might be major transporters responsible for the pharmacokinetics and drug–drug interaction of TM‐25659, although their contribution to in vivo pharmacokinetics needs to be further investigated. Copyright © 2013 John Wiley & Sons, Ltd." @default.
• W2099802056 created "2016-06-24" @default.
• W2099802056 creator A5014699929 @default.
• W2099802056 creator A5020233523 @default.
• W2099802056 creator A5028334345 @default.
• W2099802056 creator A5036377621 @default.
• W2099802056 creator A5082774996 @default.
• W2099802056 creator A5087781317 @default.
• W2099802056 date "2013-12-18" @default.
• W2099802056 modified "2023-10-07" @default.
• W2099802056 title "Transport characteristics and transporter-based drug-drug interactions of TM-25659, a novel TAZ modulator" @default.
• W2099802056 cites W1656842517 @default.
• W2099802056 cites W1964471078 @default.
• W2099802056 cites W1983241145 @default.
• W2099802056 cites W1997601514 @default.
• W2099802056 cites W2007698657 @default.
• W2099802056 cites W2012727770 @default.
• W2099802056 cites W2018126221 @default.
• W2099802056 cites W2019834759 @default.
• W2099802056 cites W2026475103 @default.
• W2099802056 cites W2049378557 @default.
• W2099802056 cites W2073157874 @default.
• W2099802056 cites W2077796674 @default.
• W2099802056 cites W2079197876 @default.
• W2099802056 cites W2095634731 @default.
• W2099802056 cites W2099086608 @default.
• W2099802056 cites W2104075487 @default.
• W2099802056 cites W2106456872 @default.
• W2099802056 cites W2111917930 @default.
• W2099802056 cites W2116517031 @default.
• W2099802056 cites W2122023026 @default.
• W2099802056 cites W2122772601 @default.
• W2099802056 cites W2123209426 @default.
• W2099802056 cites W2123511906 @default.
• W2099802056 cites W2124775757 @default.
• W2099802056 cites W2131138924 @default.
• W2099802056 cites W2134594247 @default.
• W2099802056 cites W2159310898 @default.
• W2099802056 cites W2166226272 @default.
• W2099802056 cites W2171070365 @default.
• W2099802056 doi "https://doi.org/10.1002/bdd.1883" @default.
• W2099802056 hasPubMedId "https://pubmed.ncbi.nlm.nih.gov/24285344" @default.
• W2099802056 hasPublicationYear "2013" @default.
• W2099802056 type Work @default.
• W2099802056 sameAs 2099802056 @default.
• W2099802056 citedByCount "10" @default.
• W2099802056 countsByYear W20998020562015 @default.
• W2099802056 countsByYear W20998020562017 @default.
• W2099802056 countsByYear W20998020562018 @default.
• W2099802056 countsByYear W20998020562020 @default.
• W2099802056 countsByYear W20998020562021 @default.
• W2099802056 crossrefType "journal-article" @default.
• W2099802056 hasAuthorship W2099802056A5014699929 @default.
• W2099802056 hasAuthorship W2099802056A5020233523 @default.
• W2099802056 hasAuthorship W2099802056A5028334345 @default.
• W2099802056 hasAuthorship W2099802056A5036377621 @default.
• W2099802056 hasAuthorship W2099802056A5082774996 @default.
• W2099802056 hasAuthorship W2099802056A5087781317 @default.
• W2099802056 hasConcept C104317684 @default.
• W2099802056 hasConcept C149011108 @default.
• W2099802056 hasConcept C185592680 @default.
• W2099802056 hasConcept C193176779 @default.
• W2099802056 hasConcept C200082930 @default.
• W2099802056 hasConcept C202751555 @default.
• W2099802056 hasConcept C2780035454 @default.
• W2099802056 hasConcept C36201501 @default.
• W2099802056 hasConcept C44312359 @default.
• W2099802056 hasConcept C55493867 @default.
• W2099802056 hasConcept C62231903 @default.
• W2099802056 hasConcept C86803240 @default.
• W2099802056 hasConcept C87644729 @default.
• W2099802056 hasConcept C89311334 @default.
• W2099802056 hasConcept C98274493 @default.
• W2099802056 hasConceptScore W2099802056C104317684 @default.
• W2099802056 hasConceptScore W2099802056C149011108 @default.
• W2099802056 hasConceptScore W2099802056C185592680 @default.
• W2099802056 hasConceptScore W2099802056C193176779 @default.
• W2099802056 hasConceptScore W2099802056C200082930 @default.
• W2099802056 hasConceptScore W2099802056C202751555 @default.
• W2099802056 hasConceptScore W2099802056C2780035454 @default.
• W2099802056 hasConceptScore W2099802056C36201501 @default.
• W2099802056 hasConceptScore W2099802056C44312359 @default.
• W2099802056 hasConceptScore W2099802056C55493867 @default.
• W2099802056 hasConceptScore W2099802056C62231903 @default.
• W2099802056 hasConceptScore W2099802056C86803240 @default.
• W2099802056 hasConceptScore W2099802056C87644729 @default.
• W2099802056 hasConceptScore W2099802056C89311334 @default.
• W2099802056 hasConceptScore W2099802056C98274493 @default.
• W2099802056 hasIssue "3" @default.
• W2099802056 hasLocation W20998020561 @default.
• W2099802056 hasOpenAccess W2099802056 @default.
• W2099802056 hasPrimaryLocation W20998020561 @default.
• W2099802056 hasRelatedWork W1497012431 @default.
• W2099802056 hasRelatedWork W1997813700 @default.
• W2099802056 hasRelatedWork W2013136764 @default.
• W2099802056 hasRelatedWork W2043026248 @default.
• W2099802056 hasRelatedWork W2060484487 @default.
• W2099802056 hasRelatedWork W2081213990 @default.

• next