Science · 2003 · 628 citations · 19 references
MedicineCardiologyGeneticsCardiovascular GeneticsMedical GeneticsSignal TransductionCardiac Ion ChannelsCardiovascular Molecular PhysiologyDilated Cardiomyopathy GeneticsHeart FailureInherited CardiomyopathiesCalcium Signaling DisruptionCalcium Signaling DysregulationHeart Failure GeneticsHeart Failure Molecular MechanismsRefractory Heart FailureSarcomeric Gene MutationsTransgenic Mice
Molecular etiologies of heart failure, an emerging cardiovascular epidemic affecting 4.7 million Americans and costing 17.8 billion health-care dollars annually, remain poorly understood. Here we report that an inherited human dilated cardiomyopathy with refractory congestive heart failure is caused by a dominant Arg --> Cys missense mutation at residue 9 (R9C) in phospholamban (PLN), a transmembrane phosphoprotein that inhibits the cardiac sarcoplasmic reticular Ca2+-adenosine triphosphatase (SERCA2a) pump. Transgenic PLN(R9C) mice recapitulated human heart failure with premature death. Cellular and biochemical studies revealed that, unlike wild-type PLN, PLN(R9C) did not directly inhibit SERCA2a. Rather, PLN(R9C) trapped protein kinase A (PKA), which blocked PKA-mediated phosphorylation of wild-type PLN and in turn delayed decay of calcium transients in myocytes. These results indicate that myocellular calcium dysregulation can initiate human heart failure-a finding that may lead to therapeutic opportunities.
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