Article
Functional rescue of the constitutively internalized V2 vasopressin receptor mutant R137H by the pharmacological chaperone action of SR49059.
Molecular endocrinology (Baltimore, Md.) - 1 Aug 2004
Bernier Virginie, Lagacé Monique, Lonergan Michèle, Arthus Marie-Françoise, Bichet Daniel G, Bouvier Michel
Abstract excerpt
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...
Topics
- Animals
- Arginine
- Arrestins
- Cell Line
- Chlorocebus aethiops
- Humans
- Indoles
- Molecular Chaperones
- Mutation
- Protein Binding
- Pyrrolidines
- Receptors, Vasopressin
- beta-Arrestins