Rescue of mutant gonadotropin-releasing hormone receptor function independent of cognate receptor activity.
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ABSTRACT:
SUBMITTER: Smith E
PROVIDER: S-EPMC7324376 | biostudies-literature | 2020 Jun
REPOSITORIES: biostudies-literature
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Rescue of mutant gonadotropin-releasing hormone receptor function independent of cognate receptor activity.
Smith Emery E Janovick Jo Ann JA Bannister Thomas D TD Shumate Justin J Ganapathy Vadivel V Scampavia Louis L Spicer Timothy P TP
Scientific reports 20200629 1
Molecules that correct the folding of protein mutants, restoring their functional trafficking, are called pharmacoperones. Most are clinically irrelevant and possess intrinsic antagonist or agonist activity. Here, we identify compounds capable of rescuing the activity of mutant gonadotropin-releasing hormone receptor or GnRHR which, is sequestered within the cell and if dysfunctional leads to Hypogonadotropic Hypogonadism. To do this we screened the E90K GnRHR mutant vs. a library of 645,000 com ...[more]
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