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Matches in SemOpenAlex for { <https://semopenalex.org/work/W1976343401> ?p ?o ?g. }

• W1976343401 endingPage "1034" @default.
• W1976343401 startingPage "1029" @default.
• W1976343401 abstract "Side chain fluorination is often used to make analogs of 1,25-dihydroxyvitamin D3 [1,25(OH)2D3] resistant to degradation by 24-hydroxylase. The fluorinated nonsteroidal analogs CD578, WU515, and WY1113 have an increased prodifferentiating action on SW480-ADH colon cancer cells, which correlated with stronger induction of vitamin D receptor (VDR)-coactivator interactions and stronger repression of β-catenin/TCF activity. Cocrystallization of analog CD578 with the zebrafish (z)VDR and an SRC-1 coactivator peptide showed that the fluorine atoms of CD578 make additional contacts with Val444 and Phe448 of activation helix 12 (H12) of the zVDR and with Leu440 of the H11-H12 loop. Consequently, the SRC-1 peptide makes more contacts with the VDR-CD578 complex than with the VDR-1,25(OH)2D3 complex. These data show that fluorination not only affects degradation of an analog but can also have direct effects on H12 stabilization." @default.
• W1976343401 created "2016-06-24" @default.
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• W1976343401 date "2008-10-01" @default.
• W1976343401 modified "2023-09-25" @default.
• W1976343401 title "Superagonistic Fluorinated Vitamin D3 Analogs Stabilize Helix 12 of the Vitamin D Receptor" @default.
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• W1976343401 doi "https://doi.org/10.1016/j.chembiol.2008.08.008" @default.
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