FRET Based Assay to Discover Modulators of RyR Calcium Channels (20130323, Dr. Razvan Cornea)
A fluorescence resonance energy transfer (FRET) assay method for monitoring and testing the interactions between protein molecules in a high-throughput sample setting has been developed. The FRET system is able to test pharmaceuticals by attaching fluorescent derivatives to pairs of targeted proteins and mixing these with the drug that is being researched. This FRET method is applicable to the testing of any protein interactions.
RyR Calcium Channel Modulators
The FRET high-throughput screening method has been validated with known specific modulators of the ryanodine receptor (RyR) calcium channels. This method allows screening of large libraries of small-molecule compounds to identify inhibitors of pathological calcium leak through the RyR channels. Emerging drug candidates are expected to be effective for treatment of muscle diseases (muscular dystrophy, muscle fatigue, irregular heartbeat, heart failure), diabetes, neurological diseases (Alzheimer’s, Parkinson’s), and other pathologies associated with abnormal calcium leak through RyR. This is the first high-throughput screening technology for RyR calcium channels.
BENEFITS AND FEATURES OF RYR CALCIUM CHANNEL FRET-BASED ASSAY:
- FRET-based screening method specifically resolves compound interactions with the RyR calcium channels.
- Potential for addressing any pathology where resting intracellular calcium levels are abnormally high.
- First high-throughput assay to discover RyR modulators.
Phase of Development Proof of Concept