FRINK Linked Data Fragments server

Matches in SemOpenAlex for { <https://semopenalex.org/work/W2077134485> ?p ?o ?g. }

• W2077134485 endingPage "265" @default.
• W2077134485 startingPage "259" @default.
• W2077134485 abstract "17β-Hydroxysteroid dehydrogenase type 3 (17β-HSD3) is expressed at high levels in the testes and seminal vesicles but has also been shown to be present in prostate tissue, suggesting its potential involvement in both gonadal and non-gonadal testosterone biosynthesis. The role of 17β-HSD3 in testosterone biosynthesis makes this enzyme an attractive molecular target for small molecule inhibitors for the treatment of prostate cancer. Here we report the design of selective inhibitors of 17β-HSD3 as potential anti-cancer agents. Due to 17β-HSD3 being a membrane-bound protein a crystal structure is not yet available. A homology model of 17β-HSD3 has been built to aid structure-based drug design. This model has been used with docking studies to identify a series of lead compounds that may give an insight as to how inhibitors interact with the active site. Compound 1 was identified as a potent selective inhibitor of 17β-HSD3 with an IC50 = 700 nM resulting in the discovery of a novel lead series for further optimisation. Using our homology model as a tool for inhibitor design compound 5 was discovered as a novel potent and selective inhibitor of 17β-HSD3 with an IC50 ∼200 nM." @default.
• W2077134485 created "2016-06-24" @default.
• W2077134485 creator A5004708346 @default.
• W2077134485 creator A5004883683 @default.
• W2077134485 creator A5011660535 @default.
• W2077134485 creator A5013024538 @default.
• W2077134485 creator A5013687413 @default.
• W2077134485 creator A5017572010 @default.
• W2077134485 creator A5043165029 @default.
• W2077134485 creator A5043199638 @default.
• W2077134485 creator A5057398969 @default.
• W2077134485 creator A5070946574 @default.
• W2077134485 creator A5081964181 @default.
• W2077134485 creator A5086377022 @default.
• W2077134485 date "2009-03-01" @default.
• W2077134485 modified "2023-09-26" @default.
• W2077134485 title "The design of novel 17β-hydroxysteroid dehydrogenase type 3 inhibitors" @default.
• W2077134485 cites W1965337180 @default.
• W2077134485 cites W1986191025 @default.
• W2077134485 cites W2007245161 @default.
• W2077134485 cites W2023097049 @default.
• W2077134485 cites W2045040068 @default.
• W2077134485 cites W2050456292 @default.
• W2077134485 cites W2056021447 @default.
• W2077134485 cites W2056246315 @default.
• W2077134485 cites W2060058647 @default.
• W2077134485 cites W2082082125 @default.
• W2077134485 cites W2097382368 @default.
• W2077134485 cites W2099099776 @default.
• W2077134485 cites W2106505270 @default.
• W2077134485 cites W2123093073 @default.
• W2077134485 cites W2130479394 @default.
• W2077134485 cites W2132717858 @default.
• W2077134485 cites W2158714788 @default.
• W2077134485 cites W2168014895 @default.
• W2077134485 cites W2400271924 @default.
• W2077134485 cites W2412673684 @default.
• W2077134485 doi "https://doi.org/10.1016/j.mce.2008.08.005" @default.
• W2077134485 hasPubMedId "https://pubmed.ncbi.nlm.nih.gov/18775469" @default.
• W2077134485 hasPublicationYear "2009" @default.
• W2077134485 type Work @default.
• W2077134485 sameAs 2077134485 @default.
• W2077134485 citedByCount "26" @default.
• W2077134485 countsByYear W20771344852012 @default.
• W2077134485 countsByYear W20771344852014 @default.
• W2077134485 countsByYear W20771344852015 @default.
• W2077134485 countsByYear W20771344852017 @default.
• W2077134485 countsByYear W20771344852020 @default.
• W2077134485 countsByYear W20771344852021 @default.
• W2077134485 crossrefType "journal-article" @default.
• W2077134485 hasAuthorship W2077134485A5004708346 @default.
• W2077134485 hasAuthorship W2077134485A5004883683 @default.
• W2077134485 hasAuthorship W2077134485A5011660535 @default.
• W2077134485 hasAuthorship W2077134485A5013024538 @default.
• W2077134485 hasAuthorship W2077134485A5013687413 @default.
• W2077134485 hasAuthorship W2077134485A5017572010 @default.
• W2077134485 hasAuthorship W2077134485A5043165029 @default.
• W2077134485 hasAuthorship W2077134485A5043199638 @default.
• W2077134485 hasAuthorship W2077134485A5057398969 @default.
• W2077134485 hasAuthorship W2077134485A5070946574 @default.
• W2077134485 hasAuthorship W2077134485A5081964181 @default.
• W2077134485 hasAuthorship W2077134485A5086377022 @default.
• W2077134485 hasBestOaLocation W20771344852 @default.
• W2077134485 hasConcept C159110408 @default.
• W2077134485 hasConcept C161624437 @default.
• W2077134485 hasConcept C169627665 @default.
• W2077134485 hasConcept C181199279 @default.
• W2077134485 hasConcept C185592680 @default.
• W2077134485 hasConcept C2776317432 @default.
• W2077134485 hasConcept C2779268744 @default.
• W2077134485 hasConcept C2781067048 @default.
• W2077134485 hasConcept C41183919 @default.
• W2077134485 hasConcept C41685203 @default.
• W2077134485 hasConcept C55493867 @default.
• W2077134485 hasConcept C70721500 @default.
• W2077134485 hasConcept C71924100 @default.
• W2077134485 hasConcept C86803240 @default.
• W2077134485 hasConceptScore W2077134485C159110408 @default.
• W2077134485 hasConceptScore W2077134485C161624437 @default.
• W2077134485 hasConceptScore W2077134485C169627665 @default.
• W2077134485 hasConceptScore W2077134485C181199279 @default.
• W2077134485 hasConceptScore W2077134485C185592680 @default.
• W2077134485 hasConceptScore W2077134485C2776317432 @default.
• W2077134485 hasConceptScore W2077134485C2779268744 @default.
• W2077134485 hasConceptScore W2077134485C2781067048 @default.
• W2077134485 hasConceptScore W2077134485C41183919 @default.
• W2077134485 hasConceptScore W2077134485C41685203 @default.
• W2077134485 hasConceptScore W2077134485C55493867 @default.
• W2077134485 hasConceptScore W2077134485C70721500 @default.
• W2077134485 hasConceptScore W2077134485C71924100 @default.
• W2077134485 hasConceptScore W2077134485C86803240 @default.
• W2077134485 hasIssue "1-2" @default.
• W2077134485 hasLocation W20771344851 @default.
• W2077134485 hasLocation W20771344852 @default.
• W2077134485 hasLocation W20771344853 @default.
• W2077134485 hasLocation W20771344854 @default.
• W2077134485 hasLocation W20771344855 @default.
• W2077134485 hasLocation W20771344856 @default.

• next