Key result
Overexpression of mutant monomeric phospholamban resulted in an EC50 for Ca2+ uptake of 0.32 mumol/L versus 0.49 mumol/L for wild-type phospholamban, indicating less pronounced inhibitory effects.
Absolute Event Rate: 0.32% vs 0.49%
Pentameric assembly of phospholamban is important for mediating its optimal regulatory effects on myocardial contractility in vivo, as monomeric phospholamban has less pronounced inhibitory effects.
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Pentameric phospholamban assembly optimizes in vivo contractility regulation; challenges prior in vitro equivalence and leaves open human therapeutic relevance.
Chu et al. (1997) studied this question. Mutant (Cys41-->Phe41) phospholamban overexpression vs. Wild-type phospholamban overexpression and wild-type controls was evaluated on EC50 values for SR Ca2+ uptake. Overexpression of mutant monomeric phospholamban resulted in an EC50 for Ca2+ uptake of 0.32 mumol/L versus 0.49 mumol/L for wild-type phospholamban, indicating less pronounced inhibitory effects.
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