High-Throughput Screens to Discover Small-Molecule Modulators of Ryanodine Receptor Calcium Release Channels

Using time-resolved fluorescence resonance energy transfer (FRET), we have developed and validated the first high-throughput screening (HTS) method to discover compounds that modulate an intracellular Ca2+ channel, the ryanodine receptor (RyR), for therapeutic applications. Intracellular Ca2+ regula...

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Veröffentlicht in:	SLAS discovery 2017-02, Vol.22 (2), p.176-186
Hauptverfasser:	Rebbeck, Robyn T., Essawy, Maram M., Nitu, Florentin R., Grant, Benjamin D., Gillispie, Gregory D., Thomas, David D., Bers, Donald M., Cornea, Razvan L.
Format:	Artikel
Sprache:	eng
Schlagworte:	Calcium Signaling - drug effects Calcium Signaling - genetics Calmodulin - chemistry Calmodulin - metabolism Fluorescence Resonance Energy Transfer Humans Muscle, Skeletal - metabolism Muscle, Skeletal - pathology Nervous System Diseases - genetics Nervous System Diseases - metabolism Nervous System Diseases - pathology Protein Binding Ryanodine - metabolism Ryanodine Receptor Calcium Release Channel - chemistry Ryanodine Receptor Calcium Release Channel - genetics Ryanodine Receptor Calcium Release Channel - metabolism Tacrolimus Binding Proteins - chemistry Tacrolimus Binding Proteins - genetics Tacrolimus Binding Proteins - metabolism
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