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Myosin light chain kinase phosphorylation: regulation of the Ca2+ sensitivity of contractile elements

J T Stull1, M G Tansey, R A Word

  • 1University of Texas Southwestern Medical Center, Department of Physiology, Dallas 75235.

Insights

Smooth muscle contraction is regulated by myosin light chain kinase (MLCK) phosphorylation. Site A phosphorylation on MLCK correlates with muscle contraction, suggesting a role in desensitization to calcium.

Area of Science:

  • Biochemistry
  • Molecular Biology
  • Physiology

Background:

  • Myosin light chain kinase (MLCK) regulates smooth muscle contractility.
  • MLCK can be phosphorylated by several protein kinases, including cyclic AMP-dependent protein kinase, protein kinase C, and calmodulin-dependent protein kinase II.
  • Phosphorylation at a specific site (site A) desensitizes MLCK to Ca2+/calmodulin activation.

Purpose of the Study:

  • To investigate the role of MLCK phosphorylation in regulating smooth muscle contractility in bovine tracheal smooth muscle.
  • To determine which specific kinases phosphorylate MLCK in response to contractile stimuli.
  • To examine the correlation between site A phosphorylation and smooth muscle contraction.

Main Methods:

  • Utilized 32P-labelled bovine tracheal smooth muscle.
  • Treated tissues with contractile agents (carbachol, KCl) and non-contractile agents (isoproterenol, phorbol 12,13-dibutyrate).
  • Identified and quantified phosphopeptides of MLCK using phosphopeptide mapping.

Main Results:

  • Carbachol, KCl, isoproterenol, and phorbol 12,13-dibutyrate increased MLCK phosphorylation.
  • Six primary phosphopeptides (A-F) of MLCK were identified.
  • Site A phosphorylation occurred significantly with carbachol and KCl, correlating with smooth muscle contraction and increased Ca2+/calmodulin activation requirements.

Conclusions:

  • Cyclic AMP-dependent protein kinase and protein kinase C do not mediate smooth muscle contractility changes via site A phosphorylation of MLCK.
  • Phosphorylation of MLCK at site A, potentially by calmodulin-dependent protein kinase II, may contribute to the desensitization of smooth muscle contractile elements to Ca2+ activation.

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