High-Throughput FRET Assay Yields Allosteric SERCA Activators

Using fluorescence resonance energy transfer (FRET), we performed a high-throughput screen (HTS) in a reconstituted membrane system, seeking compounds that reverse inhibition of sarcoplasmic reticulum Ca-ATPase (SERCA) by its cardiac regulator, phospholamban (PLB). Such compounds have long been soug...

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Veröffentlicht in:	Journal of biomolecular screening 2013-01, Vol.18 (1), p.97-107
Hauptverfasser:	Cornea, Razvan L., Gruber, Simon J., Lockamy, Elizabeth L., Muretta, Joseph M., Jin, Dongzhu, Chen, Jiqiu, Dahl, Russell, Bartfai, Tamas, Zsebo, Krisztina M., Gillispie, Gregory D., Thomas, David D.
Format:	Artikel
Sprache:	eng
Schlagworte:	Allosteric properties Allosteric Regulation Animals Ca super(2+)-transporting ATPase Calcium Calcium-Binding Proteins - physiology Cardiac muscle cardiomyocytes Cells, Cultured Enzyme Activators - pharmacology Enzyme Assays Fluorescence Resonance Energy Transfer Heart Heart diseases High-Throughput Screening Assays Male Muscle contraction Myocytes, Cardiac - drug effects Myocytes, Cardiac - enzymology Myocytes, Cardiac - physiology Phospholamban Phospholipids Rabbits Rats Rats, Sprague-Dawley Sarcoplasmic reticulum Sarcoplasmic Reticulum - drug effects Sarcoplasmic Reticulum - enzymology Sarcoplasmic Reticulum Calcium-Transporting ATPases - metabolism Standard deviation Stimulation, Chemical
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