Functional rescue of the constitutively internalized V2 vasopressin receptor mutant R137H by the pharmacological chaperone action of SR49059.

@article{Bernier2004FunctionalRO,
  title={Functional rescue of the constitutively internalized V2 vasopressin receptor mutant R137H by the pharmacological chaperone action of SR49059.},
  author={Virginie Bernier and Monique Lagac{\'e} and Mich{\`e}le Lonergan and M F Arthus and Daniel Georges Bichet and Michel Bouvier},
  journal={Molecular endocrinology},
  year={2004},
  volume={18 8},
  pages={2074-84}
}
In most cases, nephrogenic diabetes insipidus results from mutations in the V2 vasopressin receptor (V2R) gene that cause intracellular retention of improperly folded receptors. We previously reported that cell permeable V2R antagonists act as pharmacological chaperones that rescue folding, trafficking, and function of several V2R mutants. More recently, the vasopressin antagonist, SR49059, was found to be therapeutically active in nephrogenic diabetes insipidus patients. Three of the patients… CONTINUE READING

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