A chemical, genetic, and structural analysis of the nuclear bile acid receptor FXR.

@article{Downes2003ACG,
  title={A chemical, genetic, and structural analysis of the nuclear bile acid receptor FXR.},
  author={Michael Frank Downes and Mark A. Verdecia and Anthony J. Roecker and Robert M Hughes and John B. Hogenesch and Heidi R. Kast-Woelbern and M. E. Bowman and Jean-Luc Ferrer and Andrew M. Anisfeld and Peter A. Edwards and John M Rosenfeld and Jacqueline G.A Alvarez and Joseph P Noel and Kyriacos C Nicolaou and Ronald M Evans},
  journal={Molecular cell},
  year={2003},
  volume={11 4},
  pages={
          1079-92
        }
}
The farnesoid X receptor (FXR) functions as a bile acid (BA) sensor coordinating cholesterol metabolism, lipid homeostasis, and absorption of dietary fats and vitamins. However, BAs are poor reagents for characterizing FXR functions due to multiple receptor independent properties. Accordingly, using combinatorial chemistry we evolved a small molecule agonist termed fexaramine with 100-fold increased affinity relative to natural compounds. Gene-profiling experiments conducted in hepatocytes with… CONTINUE READING
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