Part:BBa_K4164002

farnesoid X receptor(FXR)

FXR is a protein from humans, it is a member of the nuclear receptor superfamily of ligand-activated transcription factors， and functions as a receptor for bile acids. It is encoded by the NR1H4 in human. FXR is expressed at high levels in the liver and intestine.

Chenodeoxycholic acid （CDCA） and other bile acids are natural ligands for FXR. Similar to other nuclear receptors, when activated, FXR translocates to the cell nucleus, forms a dimer (in this case a heterodimer with RXR) and binds to hormone response elements on DNA, which up- or down-regulates the expression of certain genes.

In order to clarify the tertiary structure of the protein after binding, we made a structural prediction of the post-binding protein.We first used SwissDock to dock small molecule CDCA with protein FXR.And the scores of corresponding energy and FullFitness of the docking protein obtained by SwissDock docking were 9.94587 and -1127.6123 respectively.This predicted docking protein provided theoretical guidance for our initial experiment.

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Fig.1 FXR+CDCA.

In our project, we took advantage of the characteristics of CDCA as the most effective activator of FXR, using FXR as the receptor, and when activated by de-sulfated CDCA-S, it will form a heterodimeric complex with the RXR, so that the linked ddRFP-A1 and ddRFP-B1 are correspondingly driven to dimerize and emit fluorescence.

Sequence and Features

Assembly Compatibility:

• 10
  COMPATIBLE WITH RFC[10]
• 12
  COMPATIBLE WITH RFC[12]
• 21
  COMPATIBLE WITH RFC[21]
• 23
  COMPATIBLE WITH RFC[23]
• 25
  COMPATIBLE WITH RFC[25]
• 1000
  INCOMPATIBLE WITH RFC[1000]

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