Fluorescence lifetime FRET assay for live-cell high-throughput screening of the cardiac SERCA pump yields multiple classes of small-molecule allosteric modulators
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Andrew R. Thompson | R. Cornea | C. Aldrich | Samantha L. Yuen | O. Roopnarine | Robyn T. Rebbeck | Philip A Bidwell | David D. Thomas | Lauren N. Roelike | A. Thompson | S. Yuen | Răzvan L. Cornea
[1] R. Cornea,et al. Interaction of DWORF with SERCA and PLB as determined by EPR spectroscopy. , 2023, Biochemical and biophysical research communications.
[2] A. Zima,et al. New N-aryl-N-alkyl-thiophene-2-carboxamide compound enhances intracellular Ca2+ dynamics by increasing SERCA2a Ca2+ pumping. , 2022, Biophysical journal.
[3] R. Cornea,et al. A Large-Scale High-Throughput Screen for Modulators of SERCA Activity , 2022, Biomolecules.
[4] J. Viskupičová,et al. Natural Polyphenols as SERCA Activators: Role in the Endoplasmic Reticulum Stress-Related Diseases , 2022, Molecules.
[5] F. Peri,et al. Highly Selective SERCA2a Activators: Preclinical Development of a Congeneric Group of First-in-Class Drug Leads against Heart Failure , 2022, Journal of medicinal chemistry.
[6] S. Dudley,et al. Reduced sarcoplasmic reticulum Ca2+ pump activity is anti-arrhythmic in ischemic cardiomyopathy. , 2022, Heart rhythm.
[7] A. R. Tupling,et al. The role of SERCA and sarcolipin in adaptive muscle remodeling. , 2022, American journal of physiology. Cell physiology.
[8] C. Barclay,et al. Ca2+ leak through ryanodine receptor 1 regulates thermogenesis in resting skeletal muscle , 2022, Proceedings of the National Academy of Sciences.
[9] Shaukatali N. Inamdar,et al. A systematic appraisal on catalytic synthesis of 1,3-oxazole derivatives: A mechanistic review on metal dependent synthesis , 2022, Synthetic Communications.
[10] David D. Thomas,et al. Sarcoplasmic Reticulum from Horse Gluteal Muscle Is Poised for Enhanced Calcium Transport , 2021, Veterinary sciences.
[11] F. Peri,et al. Istaroxime Metabolite PST3093 Selectively Stimulates SERCA2a and Reverses Disease-Induced Changes in Cardiac Function , 2021, The Journal of Pharmacology and Experimental Therapeutics.
[12] L. M. Espinoza-Fonseca,et al. Nothing Regular about the Regulins: Distinct Functional Properties of SERCA Transmembrane Peptide Regulatory Subunits , 2021, International journal of molecular sciences.
[13] I. Palchetti,et al. Stimulation of Ca2+‐ATPase Transport Activity by a Small‐Molecule Drug , 2021, ChemMedChem.
[14] M. J. Lemieux,et al. Dwarf open reading frame (DWORF) is a direct activator of the sarcoplasmic reticulum calcium pump SERCA , 2021, eLife.
[15] D. Bers,et al. Increasing SERCA function promotes initiation of calcium sparks and breakup of calcium waves , 2021, The Journal of physiology.
[16] J. Kira,et al. Pharmacological activation of SERCA ameliorates dystrophic phenotypes in dystrophin-deficient mdx mice , 2021, Human molecular genetics.
[17] Daniel R. Stroik,et al. The transmembrane peptide DWORF activates SERCA2a via dual mechanisms , 2021, The Journal of biological chemistry.
[18] G. Roti,et al. Targeting oncogenic Notch signaling with SERCA inhibitors , 2021, Journal of Hematology & Oncology.
[19] David D. Thomas,et al. Novel drug discovery platform for spinocerebellar ataxia, using fluorescence technology targeting β-III-spectrin , 2020, The Journal of biological chemistry.
[20] David D. Thomas,et al. Discovery of small molecule inhibitors of huntingtin exon 1 aggregation by FRET-based high-throughput screening in living cells. , 2020, ACS chemical neuroscience.
[21] L. M. Espinoza-Fonseca,et al. Linking Biochemical and Structural States of SERCA: Achievements, Challenges, and New Opportunities , 2020, International journal of molecular sciences.
[22] Tory M. Schaaf,et al. Live-Cell Cardiac-Specific High-Throughput Screening Platform for Drug-Like Molecules That Enhance Ca2+ Transport , 2020, Cells.
[23] M. Periasamy,et al. Uncoupling of sarcoendoplasmic reticulum calcium ATPase pump activity by sarcolipin as the basis for muscle non-shivering thermogenesis , 2020, Philosophical Transactions of the Royal Society B.
[24] Tory M. Schaaf,et al. Noncompetitive inhibitors of TNFR1 probe conformational activation states , 2019, Science Signaling.
[25] Tory M. Schaaf,et al. Red-Shifted FRET Biosensors for High-Throughput Fluorescence Lifetime Screening , 2018, Biosensors.
[26] E. Olson,et al. The DWORF micropeptide enhances contractility and prevents heart failure in a mouse model of dilated cardiomyopathy , 2018, eLife.
[27] Tory M. Schaaf,et al. Targeting protein-protein interactions for therapeutic discovery via FRET-based high-throughput screening in living cells , 2018, Scientific Reports.
[28] R. Dahl,et al. A new target for Alzheimer's disease: A small molecule SERCA activator is neuroprotective in vitro and improves memory and cognition in APP/PS1 mice. , 2018, Bioorganic & medicinal chemistry letters.
[29] A. Zima,et al. Redistribution of SERCA calcium pump conformers during intracellular calcium signaling , 2018, The Journal of Biological Chemistry.
[30] T. Ruf,et al. Muscle Non-shivering Thermogenesis and Its Role in the Evolution of Endothermy , 2017, Front. Physiol..
[31] Tory M. Schaaf,et al. Spectral Unmixing Plate Reader: High-Throughput, High-Precision FRET Assays in Living Cells , 2017, SLAS discovery : advancing life sciences R & D.
[32] Tory M. Schaaf,et al. High-Throughput Spectral and Lifetime-Based FRET Screening in Living Cells to Identify Small-Molecule Effectors of SERCA , 2016, SLAS discovery : advancing life sciences R & D.
[33] B. Engelen,et al. Characterization of sarcoplasmic reticulum Ca2+ ATPase pumps in muscle of patients with myotonic dystrophy and with hypothyroid myopathy , 2016, Neuromuscular Disorders.
[34] Stephen C. Cannon,et al. A peptide encoded by a transcript annotated as long noncoding RNA enhances SERCA activity in muscle , 2016, Science.
[35] S. Maurya,et al. Sarcolipin is a novel regulator of muscle metabolism and obesity. , 2015, Pharmacological research.
[36] E. Calabrese,et al. HORMESIS: A Fundamental Concept with Widespread Biological and Biomedical Applications , 2015, Gerontology.
[37] M. Neil,et al. Correction Approach for Delta Function Convolution Model Fitting of Fluorescence Decay Data in the Case of a Monoexponential Reference Fluorophore , 2015, Journal of Fluorescence.
[38] J. T. Njardarson,et al. Analysis of the structural diversity, substitution patterns, and frequency of nitrogen heterocycles among U.S. FDA approved pharmaceuticals. , 2014, Journal of medicinal chemistry.
[39] Peter Willett,et al. The Calculation of Molecular Structural Similarity: Principles and Practice , 2014, Molecular informatics.
[40] D. Bers. Cardiac sarcoplasmic reticulum calcium leak: basis and roles in cardiac dysfunction. , 2014, Annual review of physiology.
[41] L. A. Anwer,et al. Cardiac SERCA2A/B: therapeutic targets for heart failure. , 2014, European journal of pharmacology.
[42] Tory M. Schaaf,et al. Discovery of Enzyme Modulators via High-Throughput Time-Resolved FRET in Living Cells , 2014, Journal of biomolecular screening.
[43] David D. Thomas,et al. Phosphorylated phospholamban stabilizes a compact conformation of the cardiac calcium-ATPase. , 2013, Biophysical journal.
[44] Jiqiu Chen,et al. High-Throughput FRET Assay Yields Allosteric SERCA Activators , 2013, Journal of biomolecular screening.
[45] David D. Thomas,et al. 2-Color Calcium Pump Reveals Closure of the Cytoplasmic Headpiece with Calcium Binding , 2012, PloS one.
[46] R. Hajjar,et al. Modulation of Cardiac Contractility by the Phopholamban/SERCA2a Regulatome , 2012, Circulation research.
[47] R. Hajjar,et al. Calcium Cycling Proteins and Their Association With Heart Failure , 2011, Clinical pharmacology and therapeutics.
[48] J. East,et al. A diversity of SERCA Ca2+ pump inhibitors. , 2011, Biochemical Society transactions.
[49] Yiqun Cao,et al. ChemMine tools: an online service for analyzing and clustering small molecules , 2011, Nucleic Acids Res..
[50] J. Baell,et al. New substructure filters for removal of pan assay interference compounds (PAINS) from screening libraries and for their exclusion in bioassays. , 2010, Journal of medicinal chemistry.
[51] R. Hajjar,et al. Interplay between impaired calcium regulation and insulin signaling abnormalities in diabetic cardiomyopathy , 2008, Nature Clinical Practice Cardiovascular Medicine.
[52] M. Rocchetti,et al. Modulation of Sarcoplasmic Reticulum Function by PST2744 [Istaroxime; (E,Z)-3-((2-Aminoethoxy)imino) Androstane-6,17-dione Hydrochloride)] in a Pressure-Overload Heart Failure Model , 2008, Journal of Pharmacology and Experimental Therapeutics.
[53] A. Schuffenhauer,et al. Charting biologically relevant chemical space: a structural classification of natural products (SCONP). , 2005, Proceedings of the National Academy of Sciences of the United States of America.
[54] Herbert Waldmann,et al. Design of compound libraries based on natural product scaffolds and protein structure similarity clustering (PSSC). , 2005, Molecular bioSystems.
[55] H. Wolfson,et al. Access the most recent version at doi: 10.1110/ps.21302 References , 2001 .
[56] Thomas D. Y. Chung,et al. A Simple Statistical Parameter for Use in Evaluation and Validation of High Throughput Screening Assays , 1999, Journal of biomolecular screening.
[57] D. Maclennan,et al. Measurement of Resting Cytosolic Ca2+ Concentrations and Ca2+ Store Size in HEK-293 Cells Transfected with Malignant Hyperthermia or Central Core Disease Mutant Ca2+ Release Channels* , 1999, The Journal of Biological Chemistry.
[58] J. Ludden,et al. Principles and Practice , 1998, Community-based Learning and Social Movements.
[59] G. Inesi,et al. Variable Stoichiometric Efficiency of Ca2+ and Sr2+ Transport by the Sarcoplasmic Reticulum ATPase (*) , 1995, The Journal of Biological Chemistry.
[60] E. Racker,et al. A coupling factor from sarcoplasmic reticulum required for the translocation of Ca2+ ions in a reconstituted Ca2+ATPase pump. , 1975, The Journal of biological chemistry.
[61] Tory M. Schaaf,et al. Fluorescence-Based TNFR1 Biosensor for Monitoring Receptor Structural and Conformational Dynamics and Discovery of Small Molecule Modulators. , 2021, Methods in molecular biology.
[62] M. Gheorghiade,et al. Combining SERCA2a activation and Na-K ATPase inhibition: a promising new approach to managing acute heart failure syndromes with low cardiac output. , 2011, Discovery medicine.
[63] D. Bers,et al. Cardiac myocytes Ca2+ and Na+ regulation in normal and failing hearts. , 2006, Journal of pharmacological sciences.
[64] D. Bers,et al. Roles of Diastolic Leak and Ca Transport , 2003 .
[65] D. Bers,et al. Sarcoplasmic Reticulum Ca 2 and Heart Failure Roles of Diastolic Leak and Ca 2 Transport , 2003 .
[66] F. Lombardo,et al. Experimental and computational approaches to estimate solubility and permeability in drug discovery and development settings. , 2001, Advanced drug delivery reviews.