A high throughput screening assay to identify bone morphogenic protein (BMP) modulators.
- Homogeneous proximity-induced interaction method.
- Robust, highly sensitive, easy to use method of monitoring BMP interaction.
- Characterization of potential BMP modulators for therapeutic development.
The BMP/BMP receptor interaction represents an important target for the discovery of novel therapeutic agents for the treatment of various BMP-signaling mediated diseases. Emory researchers have shown that BMP is a potent pro-inflammatory cytokine that causes hypertension and atherosclerosis in mice. In addition, they have demonstrated that these BMP-induced conditions could be completely prevented by treating mice with the BMP inhibitor noggin. In order to discover noggin-like small molecule inhibitors, a homogeneous proximity-induced interaction method to monitor the association of BMP and its receptor has been developed. A BMP/BMP receptor based fluorescence resonance energy transfer (FRET) technology has been developed that is highly sensitive and has a high density plate format. The FRET signal can be inhibited by noggin in a dose-dependent manner, which validates this assay for the identification of BMP modulators. The assay features a one-step "mix-and-read" method and is particularly suited for use in high throughput screening or ultra high throughput screening for BMP modulators.
Developmental Stage & Potential Market
- This technology has been reduced to practice and has successfully identified four highly active, potential BMP inhibitors.
- Due to the broad spectrum of activity that BMP inhibitors exhibit, a technology that is able to effectively identify potential inhibitors is needed.