FRINK Linked Data Fragments server

Matches in SemOpenAlex for { <https://semopenalex.org/work/W4207048009> ?p ?o ?g. }

• W4207048009 endingPage "109822" @default.
• W4207048009 startingPage "109822" @default.
• W4207048009 abstract "Testosterone depletion is a common aim in the treatment of hormone-dependent prostate cancer, since the steroid boosts the tumor's proliferation. Therefore, inhibition of 17β-hydroxysteroid dehydrogenase type 3 (17βHSD3), which catalyzes the carbonyl reduction of androstenedione to testosterone, represents an expedient therapeutic drug target. Among the compounds targeting 17βHSD3, tetrahydrodibenzazocines have been reported to be highly potent inhibitors. Thus, we hypothesized that structural analogs to the tetrahydrodibenzazocine scaffold, namely diazocines, which contain an azo group instead of the ethylene moiety, are also able to inhibit 17βHSD3. Diazocines consist of a photoresponsive core and can be isomerized from Z into E configuration by irradiation with a specific wavelength. In the present study, 17βHSD3 inhibition by diazocine photoisomers was examined in transfected human embryonic kidney 293 cells (HEK-293) and isolated microsomes. For this purpose, cells or microsomes were treated with androstenedione and incubated for 2 or 24 h in the presence or absence of irradiated and non-irradiated diazocines. Testosterone formation was determined by uHPLC. We report a weak inhibition of 17βHSD3 activity by diazocines in HEK-293 cells and microsomes. Furthermore, we found no significant difference between samples treated with irradiated and non-irradiated diazocines in terms of inhibition. However, we detected a new compound by HPLC analysis, which only appeared in light-treated samples, indicating a chemical modification of the photoswitched diazocines, presumably rendering them ineffective. Further investigations revealed that this modification occurs in the presence of reducing agents like dithiothreitol and glutathione. A preliminary mass-spectrometric analysis suggests that the N-N double bond is reduced, resulting in a dianiline derivative. Nevertheless, optimized photoswitchable diazocine derivatives, which are stable in a cellular environment, might serve as potent 17βHSD3 inhibitors, effective only in irradiated tissue." @default.
• W4207048009 created "2022-01-26" @default.
• W4207048009 creator A5008529161 @default.
• W4207048009 creator A5008943710 @default.
• W4207048009 creator A5013397489 @default.
• W4207048009 creator A5023912907 @default.
• W4207048009 creator A5043827878 @default.
• W4207048009 creator A5050683211 @default.
• W4207048009 date "2022-02-01" @default.
• W4207048009 modified "2023-10-17" @default.
• W4207048009 title "Reduction of photoswitched, nitrogen bridged N-acetyl diazocines limits inhibition of 17βHSD3 activity in transfected human embryonic kidney 293 cells" @default.
• W4207048009 cites W1580968270 @default.
• W4207048009 cites W1699447737 @default.
• W4207048009 cites W1874711993 @default.
• W4207048009 cites W1965372133 @default.
• W4207048009 cites W1969814274 @default.
• W4207048009 cites W1972178526 @default.
• W4207048009 cites W1985280569 @default.
• W4207048009 cites W1985588649 @default.
• W4207048009 cites W1994324783 @default.
• W4207048009 cites W2006746802 @default.
• W4207048009 cites W2009423060 @default.
• W4207048009 cites W2031168104 @default.
• W4207048009 cites W2031475842 @default.
• W4207048009 cites W2041146811 @default.
• W4207048009 cites W2043152591 @default.
• W4207048009 cites W2059617884 @default.
• W4207048009 cites W2060058647 @default.
• W4207048009 cites W2095472314 @default.
• W4207048009 cites W2095565245 @default.
• W4207048009 cites W2102377211 @default.
• W4207048009 cites W2152997446 @default.
• W4207048009 cites W2158231251 @default.
• W4207048009 cites W2159517143 @default.
• W4207048009 cites W2168014895 @default.
• W4207048009 cites W2185460746 @default.
• W4207048009 cites W2213710629 @default.
• W4207048009 cites W2312858765 @default.
• W4207048009 cites W2412673684 @default.
• W4207048009 cites W2486721152 @default.
• W4207048009 cites W2536358996 @default.
• W4207048009 cites W2734363074 @default.
• W4207048009 cites W2769426045 @default.
• W4207048009 cites W2885738414 @default.
• W4207048009 cites W2914368040 @default.
• W4207048009 cites W2965029365 @default.
• W4207048009 cites W3130955206 @default.
• W4207048009 cites W3135542571 @default.
• W4207048009 cites W99134297 @default.
• W4207048009 doi "https://doi.org/10.1016/j.cbi.2022.109822" @default.
• W4207048009 hasPubMedId "https://pubmed.ncbi.nlm.nih.gov/35074339" @default.
• W4207048009 hasPublicationYear "2022" @default.
• W4207048009 type Work @default.
• W4207048009 citedByCount "4" @default.
• W4207048009 countsByYear W42070480092023 @default.
• W4207048009 crossrefType "journal-article" @default.
• W4207048009 hasAuthorship W4207048009A5008529161 @default.
• W4207048009 hasAuthorship W4207048009A5008943710 @default.
• W4207048009 hasAuthorship W4207048009A5013397489 @default.
• W4207048009 hasAuthorship W4207048009A5023912907 @default.
• W4207048009 hasAuthorship W4207048009A5043827878 @default.
• W4207048009 hasAuthorship W4207048009A5050683211 @default.
• W4207048009 hasConcept C104317684 @default.
• W4207048009 hasConcept C134018914 @default.
• W4207048009 hasConcept C145103041 @default.
• W4207048009 hasConcept C174510640 @default.
• W4207048009 hasConcept C181199279 @default.
• W4207048009 hasConcept C185592680 @default.
• W4207048009 hasConcept C2776683971 @default.
• W4207048009 hasConcept C2777824588 @default.
• W4207048009 hasConcept C2777911890 @default.
• W4207048009 hasConcept C2780091579 @default.
• W4207048009 hasConcept C54009773 @default.
• W4207048009 hasConcept C55493867 @default.
• W4207048009 hasConcept C71315377 @default.
• W4207048009 hasConcept C86803240 @default.
• W4207048009 hasConcept C87644729 @default.
• W4207048009 hasConceptScore W4207048009C104317684 @default.
• W4207048009 hasConceptScore W4207048009C134018914 @default.
• W4207048009 hasConceptScore W4207048009C145103041 @default.
• W4207048009 hasConceptScore W4207048009C174510640 @default.
• W4207048009 hasConceptScore W4207048009C181199279 @default.
• W4207048009 hasConceptScore W4207048009C185592680 @default.
• W4207048009 hasConceptScore W4207048009C2776683971 @default.
• W4207048009 hasConceptScore W4207048009C2777824588 @default.
• W4207048009 hasConceptScore W4207048009C2777911890 @default.
• W4207048009 hasConceptScore W4207048009C2780091579 @default.
• W4207048009 hasConceptScore W4207048009C54009773 @default.
• W4207048009 hasConceptScore W4207048009C55493867 @default.
• W4207048009 hasConceptScore W4207048009C71315377 @default.
• W4207048009 hasConceptScore W4207048009C86803240 @default.
• W4207048009 hasConceptScore W4207048009C87644729 @default.
• W4207048009 hasLocation W42070480091 @default.
• W4207048009 hasLocation W42070480092 @default.
• W4207048009 hasOpenAccess W4207048009 @default.
• W4207048009 hasPrimaryLocation W42070480091 @default.
• W4207048009 hasRelatedWork W115085320 @default.
• W4207048009 hasRelatedWork W1965374807 @default.

• next