Measuring GPER Agonism, Antagonism, and Inverse Agonism Using a High-Throughput Screening Assay

SLU ID 17-007 | Novel High-Throughput Calcium Mobilization Screening Assay To Determine Therapeutic Value Of A Novel Series Of GPER Ligands

Background

A novel high-throughput screening (HTS) assay for the G protein-coupled estrogen receptor (GPER) activity has been designed. Previous screening techniques have utilized virtual screening, radio-ligand binding, and low-throughput platforms to identify ligands that may possess therapeutic value. The development of a HTS platform has the ability to drive the discovery of GPER ligands to an immeasurable and unprecedented level.

Overview

Researchers at Saint Louis University have developed a high-throughput screening assay for GPER activity. This HTP assay provides a platform to measure GPER agonism, antagonism, and inverse agonism. Concurrently, the researchers derived a novel series of compounds from molecular modeling that are selective GPER ligands.

Benefits

The potential benefits of this technology include:

• Increasing the ability to perform large scale screenings

• Increasing the ability to perform triplicates or more on a single plate

• Minimizing the time it takes to screen compounds

• Minimizing the cost of screening compounds

Applications

The potential applications of this technology include the development of treatments for a variety of diseases such as:

• gallstone disease

• leukemia

• breast cancer

• diseases characterized by neuronal cell death

Opportunity

Saint Louis University is seeking partners to further develop and commercialize this technology.