FRINK Linked Data Fragments server

Matches in SemOpenAlex for { <https://semopenalex.org/work/W1575452818> ?p ?o ?g. }

• W1575452818 endingPage "359" @default.
• W1575452818 startingPage "348" @default.
• W1575452818 abstract "Detecting prostate cancer before spreading or predicting a favorable therapy are challenging issues for impacting patient's survival. Presently, 2-[(18) F]-fluoro-2-deoxy-D-glucose ((18) F-FDG) and/or (18) F-fluorocholine ((18) F-FCH) are the generally used PET-tracers in oncology yet do not emphasize the T877A androgen receptor (AR) mutation being exclusively present in cancerous tissue and escaping androgen deprivation treatment.We designed and synthesized fluorinated 5α-dihydrotestosterone (DHT) derivatives to target T877A-AR. We performed binding assays to select suitable candidates using COS-7 cells transfected with wild-type or T877A AR (WT-AR, T877A-AR) expressing plasmids and investigated cellular uptake of candidate (18) F-RB390. Stability, biodistribution analyses and PET-Imaging were assessed by injecting (18) F-RB390 (10MBq), with and without co-injection of an excess of unlabeled DHT in C4-2 and PC-3 tumor bearing male SCID mice (n = 12).RB390 presented a higher relative binding affinity (RBA) (28.1%, IC50 = 32 nM) for T877A-AR than for WT-AR (1.7%, IC50 = 357 nM) related to DHT (RBA = 100%). A small fraction of (18) F-RB390 was metabolized when incubated with murine liver homogenate or human blood for 3 hr. The metabolite of RB390, 3-hydroxysteroid RB448, presented similar binding characteristics as RB390. (18) F-RB390 but not (18) F-FDG or (18) F-FCH accumulated 2.5× more in COS-7 cells transfected with pSG5AR-T877A than with control plasmid. Accumulation was reduced with an excess of DHT. PET/CT imaging and biodistribution studies revealed a significantly higher uptake of (18) F-RB390 in T877A mutation positive xenografts compared to PC-3 control tumors. This effect was blunted with DHT.Given the differential binding capacity and the favorable radioactivity pattern, (18) F-RB390 represents the portrayal of the first imaging ligand with predictive potential for mutant T877A-AR in prostate cancer for guiding therapy. Prostate 75:348-359, 2015. © 2014 Wiley Periodicals, Inc." @default.
• W1575452818 created "2016-06-24" @default.
• W1575452818 creator A5000437566 @default.
• W1575452818 creator A5011006711 @default.
• W1575452818 creator A5015837947 @default.
• W1575452818 creator A5051282495 @default.
• W1575452818 creator A5060743045 @default.
• W1575452818 creator A5077967152 @default.
• W1575452818 creator A5081097788 @default.
• W1575452818 creator A5090140814 @default.
• W1575452818 date "2014-10-30" @default.
• W1575452818 modified "2023-10-14" @default.
• W1575452818 title "18 F-RB390: Innovative ligand for imaging the T877A androgen receptor mutant in prostate cancer via positron emission tomography (PET)" @default.
• W1575452818 cites W1971183831 @default.
• W1575452818 cites W1971456977 @default.
• W1575452818 cites W1975691556 @default.
• W1575452818 cites W1985588649 @default.
• W1575452818 cites W2009782491 @default.
• W1575452818 cites W2009898684 @default.
• W1575452818 cites W2016333647 @default.
• W1575452818 cites W2017757468 @default.
• W1575452818 cites W2030042532 @default.
• W1575452818 cites W2030819637 @default.
• W1575452818 cites W2038103236 @default.
• W1575452818 cites W2041513939 @default.
• W1575452818 cites W2050551827 @default.
• W1575452818 cites W2051743481 @default.
• W1575452818 cites W2059546636 @default.
• W1575452818 cites W2061963051 @default.
• W1575452818 cites W2069576182 @default.
• W1575452818 cites W2082843485 @default.
• W1575452818 cites W2096613911 @default.
• W1575452818 cites W2113544380 @default.
• W1575452818 cites W2123161437 @default.
• W1575452818 cites W2125038032 @default.
• W1575452818 cites W2143639224 @default.
• W1575452818 cites W2143917623 @default.
• W1575452818 cites W2146104410 @default.
• W1575452818 cites W2151922331 @default.
• W1575452818 cites W2160534562 @default.
• W1575452818 cites W25487609 @default.
• W1575452818 doi "https://doi.org/10.1002/pros.22919" @default.
• W1575452818 hasPubMedId "https://pubmed.ncbi.nlm.nih.gov/25358634" @default.
• W1575452818 hasPublicationYear "2014" @default.
• W1575452818 type Work @default.
• W1575452818 sameAs 1575452818 @default.
• W1575452818 citedByCount "3" @default.
• W1575452818 countsByYear W15754528182015 @default.
• W1575452818 countsByYear W15754528182016 @default.
• W1575452818 crossrefType "journal-article" @default.
• W1575452818 hasAuthorship W1575452818A5000437566 @default.
• W1575452818 hasAuthorship W1575452818A5011006711 @default.
• W1575452818 hasAuthorship W1575452818A5015837947 @default.
• W1575452818 hasAuthorship W1575452818A5051282495 @default.
• W1575452818 hasAuthorship W1575452818A5060743045 @default.
• W1575452818 hasAuthorship W1575452818A5077967152 @default.
• W1575452818 hasAuthorship W1575452818A5081097788 @default.
• W1575452818 hasAuthorship W1575452818A5090140814 @default.
• W1575452818 hasConcept C104317684 @default.
• W1575452818 hasConcept C116569031 @default.
• W1575452818 hasConcept C121608353 @default.
• W1575452818 hasConcept C126322002 @default.
• W1575452818 hasConcept C153911025 @default.
• W1575452818 hasConcept C170493617 @default.
• W1575452818 hasConcept C185592680 @default.
• W1575452818 hasConcept C202751555 @default.
• W1575452818 hasConcept C2775842073 @default.
• W1575452818 hasConcept C2777477808 @default.
• W1575452818 hasConcept C2777752497 @default.
• W1575452818 hasConcept C2777807558 @default.
• W1575452818 hasConcept C2777899217 @default.
• W1575452818 hasConcept C2777911890 @default.
• W1575452818 hasConcept C2779881493 @default.
• W1575452818 hasConcept C2780192828 @default.
• W1575452818 hasConcept C2989005 @default.
• W1575452818 hasConcept C3017724952 @default.
• W1575452818 hasConcept C502942594 @default.
• W1575452818 hasConcept C54009773 @default.
• W1575452818 hasConcept C55493867 @default.
• W1575452818 hasConcept C61367390 @default.
• W1575452818 hasConcept C71315377 @default.
• W1575452818 hasConcept C71924100 @default.
• W1575452818 hasConcept C86803240 @default.
• W1575452818 hasConceptScore W1575452818C104317684 @default.
• W1575452818 hasConceptScore W1575452818C116569031 @default.
• W1575452818 hasConceptScore W1575452818C121608353 @default.
• W1575452818 hasConceptScore W1575452818C126322002 @default.
• W1575452818 hasConceptScore W1575452818C153911025 @default.
• W1575452818 hasConceptScore W1575452818C170493617 @default.
• W1575452818 hasConceptScore W1575452818C185592680 @default.
• W1575452818 hasConceptScore W1575452818C202751555 @default.
• W1575452818 hasConceptScore W1575452818C2775842073 @default.
• W1575452818 hasConceptScore W1575452818C2777477808 @default.
• W1575452818 hasConceptScore W1575452818C2777752497 @default.
• W1575452818 hasConceptScore W1575452818C2777807558 @default.
• W1575452818 hasConceptScore W1575452818C2777899217 @default.
• W1575452818 hasConceptScore W1575452818C2777911890 @default.
• W1575452818 hasConceptScore W1575452818C2779881493 @default.

• next