Article
A phenotypic high throughput screening assay for the identification of pharmacoperones for the gonadotropin releasing hormone receptor.
Assay and drug development technologies - 1 May 2014
Conn P Michael, Smith Emery, Spicer Timothy, Chase Peter, Scampavia Louis, Janovick Jo Ann
Abstract excerpt
We describe a phenotypic high throughput screening (HTS) calcium flux assay designed to identify pharmacoperones for the gonadotropin releasing hormone receptor (GnRHR). Pharmacoperones are target-specific, small molecules that diffuse into cells, rescue misfolded protein mutants, and restore them to function. Rescue is based on correcting the trafficking of mutants that would otherwise be retained in the...
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