Impact of clinically relevant mutations on the pharmacoregulation and signaling bias of the calcium-sensing receptor by positive and negative allosteric modulators.

@article{Leach2013ImpactOC,
  title={Impact of clinically relevant mutations on the pharmacoregulation and signaling bias of the calcium-sensing receptor by positive and negative allosteric modulators.},
  author={Katie Leach and Adriel Wen and Anna Evelyn Cook and Patrick M. Sexton and Arthur D. Conigrave and Arthur Christopoulos},
  journal={Endocrinology},
  year={2013},
  volume={154 3},
  pages={
          1105-16
        }
}
Cinacalcet is predominantly used to treat secondary hyperparathyroidism due to end-stage renal failure, but, more recently, its potential clinical efficacy in treating patients with loss-of-function mutations in the calcium-sensing receptor (CaSR) has been recognized. Many clinically relevant CaSR mutations are located in the heptahelical membrane spanning and extracellular loop regions of the receptor, where allosteric modulators are predicted to bind. The aim of the present study was to… CONTINUE READING
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