Key result
Omecamtiv rescues myosin VI D179Y mutant processivity by slowing actin-independent phosphate release.
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In vitro rescue of mutant myosin VI does not change practice; leaves open extension of omecamtiv to noncardiac myosins.
Mutations in the reverse-direction myosin, myosin VI, are associated with deafness in humans and mice. A myosin VI deafness mutation, D179Y, which is in the transducer of the motor, uncoupled the release of the ATP hydrolysis product, inorganic phosphate (Pi), from dependency on actin binding and destroyed the ability of single dimeric molecules to move processively on actin filaments. We observed that processive movement is rescued if ATP is added to the mutant dimer following binding of both heads to actin in the absence of ATP, demonstrating that the mutation selectively destroys the initiation of processive runs at physiological ATP levels. A drug (omecamtiv) that accelerates the actin-activated activity of cardiac myosin was able to rescue processivity of the D179Y mutant dimers at physiological ATP concentrations by slowing the actin-independent release of Pi. Thus, it may be possible to create myosin VI-specific drugs that rescue the function of deafness-causing mutations.
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Pylypenko et al. (2015) studied Deafness (myosin VI mutation). Omecamtiv was evaluated on Processive movement on actin filaments. Omecamtiv rescued the processivity of myosin VI D179Y mutant dimers at physiological ATP concentrations by slowing actin-independent release of inorganic phosphate.
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