Article
Inverse agonist abolishes desensitization of a constitutively active mutant of thyrotropin-releasing hormone receptor: role of cellular calcium and protein kinase C.
British journal of pharmacology - 1 Mar 1999
Grimberg H, Zaltsman I, Lupu-Meiri M, Gershengorn M C, Oron Y
Abstract excerpt
1. C335Stop is a constitutively active mutant of the TRH receptor (TRH-R). To investigate the mechanism of the decreased responsiveness of C335Stop TRH-R, we studied cellular Ca2+ concentrations ([Ca2+]i) in AtT20 cells stably transfected with C335Stop TRH-R cDNA, or Ca2+-activated chloride currents in Xenopus laevis oocytes expressing this mutant receptor after injection of cRNA. The competitive TRH-R binding...
Topics
- Animals
- Anti-Anxiety Agents
- Benzodiazepines
- Calcium
- Mutation
- Oocytes
- Protein Kinase C
- Receptors, Thyrotropin-Releasing Hormone
- Thyrotropin-Releasing Hormone
- Tumor Cells, Cultured
- Xenopus laevis