Conformational modulation of the farnesoid X receptor by prenylflavonoids: Insights from hydrogen deuterium exchange mass spectrometry (HDX-MS), fluorescence titration and molecular docking studies
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- 作者：Liping Yanga ; David Brodericka ; Yan Campbelld ; f ; Adrian F. Gombartd ; f ; Jan F. Stevensd ; e ; Yuan Jiangc ; Victor L. Hsuf ; ; William H. Bissonb ; ; Claudia S. Maiera ; d ; Claudia.maier@oregonstate.edu" class="auth_mail" title="E-mail the corresponding author
- 关键词：FXR ; farnesoid X receptor ; HDX-MS ; hydrogen deuterium exchange mass spectrometry ; MetS ; metabolic syndromes ; SHP ; small heterodimer partner ; BSEP ; bile salt export pump ; LBD ; ligand binding domain ; XN ; xanthohumol ; IX ; isoxanthohumol ; 8-PN ; 8-prenylnarigenin ; TX ; tetrahydroxanthohumol ; DBD ; DNA-binding domain ; CDCA ; chenodeoxycholic acid ; GG ; guggulsterone ; IPTG ; isopropyl-β-d-thiogalactopyranoside ; DMSO ; dimethylsulfoxide ; HSA ; human serum albumin ; PLGS ; ProteinLynx Global Server
- 刊名：Biochimica et Biophysica Acta (BBA) - Proteins and Proteomics
- 出版年：2016
- 出版时间：December 2016
- 年：2016
- 卷：1864
- 期：12
- 页码：1667-1677
- 全文大小：1830 K
文摘
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Solution-phase HDX dynamics of FXR LBD interactions with prenylflavonoids
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Fluorescence spectroscopy support interaction of prenylflavonoids with FXR LBD.
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Molecular docking reveals site of interactions of prenylflavonoids with FXR LBD.
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Prenylflavonoids interacts with the canonical site of the FXR LBD.
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Prenylflavonoids are bona fide ligands of FXR.