Calmodulin Antagonism

  • B. D. Roufogalis


Developments in the last decade formulated the concept that the Ca2+-binding protein, calmodulin, mediates many of the cellular actions of Ca2+ as a second messenger. Attempts to elucidate the role of calmodulin in cellular regulation have led to the widespread use of calmodulin antagonists, particularly the phenothiazines, first described by Weiss et al. (1974). It has become clear, however, that the compounds presently available to antagonize calmodulin have other significant biological actions at concentrations similar to those that block calmodulin. This may seriously limit their use as tools for establishing calmodulin functions, particularly in whole cells and intact tissues. In this discussion the mode of interaction of the presently available antagonists with calmodulin, and their specificity, are reviewed. Minimum criteria are established for deciding if inhibition of cellular function is associated with calmodulin antagonism.


Antipsychotic Agent Vinca Alkaloid Cyclic Nucleotide Phosphodiesterase Calmodulin Antagonist Effector Enzyme 
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Copyright information

© Springer-Verlag, Berlin Heidelberg 1985

Authors and Affiliations

  • B. D. Roufogalis
    • 1
  1. 1.Laboratory of Molecular Pharmacology, Faculty of Pharmaceutical SciencesUniversity of British ColumbiaVancouverCanada

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