Article
Structure-activity relations of successful pharmacologic chaperones for rescue of naturally occurring and manufactured mutants of the gonadotropin-releasing hormone receptor.
The Journal of pharmacology and experimental therapeutics - 1 May 2003
Janovick Jo Ann, Goulet Mark, Bush Eugene, Greer Jonathan, Wettlaufer David G, Conn P Michael
Abstract excerpt
We expressed a test system of wild-type (WT) rat (r) and human (h) gonadotropin-releasing hormone (GnRH) receptors (GnRHRs), including naturally occurring (13) and manufactured (five) "loss-of-function" mutants of the GnRHR. These were used to assess the ability of different GnRH peptidomimetics to rescue defective GnRHR mutants and determine their effect on the level of membrane expression of the WT receptors....
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