FRINK Linked Data Fragments server

Matches in SemOpenAlex for { <https://semopenalex.org/work/W2897589562> ?p ?o ?g. }

• W2897589562 endingPage "145" @default.
• W2897589562 startingPage "133" @default.
• W2897589562 abstract "Tryptophan 2,3-dioxygenase (TDO) is becoming a promising therapeutic target due to its involvement in cancer and neurodegenerative diseases. Development of efficient TDO inhibitors is a prime strategy in disease treatment. However, the lack of a TDO inhibitor bioassay system slows the progress of TDO inhibitor research. Herein, an active recombinant human TDO (hTDO) was prepared under optimal expression conditions, an enzymatic assay was optimized, and two cellular assays of TDO activity were developed. Then, the potential TDO inhibitory activities of nine tryptanthrin derivatives (5a-5i) were evaluated, and the inhibitory constants (Ki), enzymatic and cellular half maximal inhibitory concentrations (IC50) were measured, and the type of inhibition was determined. The tryptanthrins had various levels of TDO inhibitory activities; tryptanthrins with a substituent at 8-position had stronger inhibitory activities than the other derivatives. Moreover, most of the compounds, except 5g and 5h, exhibited better inhibitory activities than the previously reported TDO inhibitor LM10. Furthermore, the molecular docking study of compounds 5c and 5d revealed that the O atom of the tryptanthrin ring is directed toward the heme iron (Fe) of hTDO via strong coordination interactions. These findings suggest that tryptanthrin and its derivatives have the potential to be developed as promising molecules for TDO-related target therapy." @default.
• W2897589562 created "2018-10-26" @default.
• W2897589562 creator A5012029583 @default.
• W2897589562 creator A5015001522 @default.
• W2897589562 creator A5025372417 @default.
• W2897589562 creator A5037736384 @default.
• W2897589562 creator A5046899960 @default.
• W2897589562 creator A5073785112 @default.
• W2897589562 creator A5074140465 @default.
• W2897589562 creator A5078345113 @default.
• W2897589562 date "2018-12-01" @default.
• W2897589562 modified "2023-10-13" @default.
• W2897589562 title "Tryptophan 2,3-dioxygenase inhibitory activities of tryptanthrin derivatives" @default.
• W2897589562 cites W1491975375 @default.
• W2897589562 cites W1683265163 @default.
• W2897589562 cites W1966687939 @default.
• W2897589562 cites W1972629684 @default.
• W2897589562 cites W1978203828 @default.
• W2897589562 cites W1979780595 @default.
• W2897589562 cites W1998142996 @default.
• W2897589562 cites W2008893382 @default.
• W2897589562 cites W2010145371 @default.
• W2897589562 cites W2015260577 @default.
• W2897589562 cites W2016841149 @default.
• W2897589562 cites W2023791869 @default.
• W2897589562 cites W2026679562 @default.
• W2897589562 cites W2027684176 @default.
• W2897589562 cites W2027821008 @default.
• W2897589562 cites W2031223359 @default.
• W2897589562 cites W2034521426 @default.
• W2897589562 cites W2035652454 @default.
• W2897589562 cites W2053217888 @default.
• W2897589562 cites W2053875523 @default.
• W2897589562 cites W205568925 @default.
• W2897589562 cites W2058834701 @default.
• W2897589562 cites W2071848867 @default.
• W2897589562 cites W2074495555 @default.
• W2897589562 cites W2080799304 @default.
• W2897589562 cites W2087801719 @default.
• W2897589562 cites W2103553504 @default.
• W2897589562 cites W2106041642 @default.
• W2897589562 cites W2112891363 @default.
• W2897589562 cites W2115230511 @default.
• W2897589562 cites W2122012981 @default.
• W2897589562 cites W2125600808 @default.
• W2897589562 cites W2138452800 @default.
• W2897589562 cites W2146851783 @default.
• W2897589562 cites W2147300658 @default.
• W2897589562 cites W2158207380 @default.
• W2897589562 cites W2158534713 @default.
• W2897589562 cites W2159673356 @default.
• W2897589562 cites W2165526004 @default.
• W2897589562 cites W2211473562 @default.
• W2897589562 cites W2338201176 @default.
• W2897589562 cites W2465370169 @default.
• W2897589562 cites W2550992160 @default.
• W2897589562 cites W2583073115 @default.
• W2897589562 cites W2594368015 @default.
• W2897589562 cites W2598111690 @default.
• W2897589562 cites W2768844995 @default.
• W2897589562 cites W4232180025 @default.
• W2897589562 doi "https://doi.org/10.1016/j.ejmech.2018.10.017" @default.
• W2897589562 hasPubMedId "https://pubmed.ncbi.nlm.nih.gov/30321802" @default.
• W2897589562 hasPublicationYear "2018" @default.
• W2897589562 type Work @default.
• W2897589562 sameAs 2897589562 @default.
• W2897589562 citedByCount "20" @default.
• W2897589562 countsByYear W28975895622019 @default.
• W2897589562 countsByYear W28975895622020 @default.
• W2897589562 countsByYear W28975895622021 @default.
• W2897589562 countsByYear W28975895622022 @default.
• W2897589562 countsByYear W28975895622023 @default.
• W2897589562 crossrefType "journal-article" @default.
• W2897589562 hasAuthorship W2897589562A5012029583 @default.
• W2897589562 hasAuthorship W2897589562A5015001522 @default.
• W2897589562 hasAuthorship W2897589562A5025372417 @default.
• W2897589562 hasAuthorship W2897589562A5037736384 @default.
• W2897589562 hasAuthorship W2897589562A5046899960 @default.
• W2897589562 hasAuthorship W2897589562A5073785112 @default.
• W2897589562 hasAuthorship W2897589562A5074140465 @default.
• W2897589562 hasAuthorship W2897589562A5078345113 @default.
• W2897589562 hasConcept C159110408 @default.
• W2897589562 hasConcept C169760540 @default.
• W2897589562 hasConcept C17077164 @default.
• W2897589562 hasConcept C181199279 @default.
• W2897589562 hasConcept C185592680 @default.
• W2897589562 hasConcept C202751555 @default.
• W2897589562 hasConcept C2777752112 @default.
• W2897589562 hasConcept C2777752497 @default.
• W2897589562 hasConcept C2778689049 @default.
• W2897589562 hasConcept C41685203 @default.
• W2897589562 hasConcept C55493867 @default.
• W2897589562 hasConcept C71240020 @default.
• W2897589562 hasConcept C71924100 @default.
• W2897589562 hasConcept C86803240 @default.
• W2897589562 hasConceptScore W2897589562C159110408 @default.
• W2897589562 hasConceptScore W2897589562C169760540 @default.
• W2897589562 hasConceptScore W2897589562C17077164 @default.

• next