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Related Experiment Videos

Cooperativity among calmodulin's drug binding sites.

J S Mills, B L Bailey, J D Johnson

    Biochemistry
    |August 27, 1985
    PubMed
    Summary

    Felodipine binding to calmodulin was investigated, revealing that antagonists like prenylamine and R24571 enhance binding affinity through allosteric mechanisms. These findings elucidate calmodulin

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    A coupled oscillator model for the origin of bimodality and multimodality.

    Chaos (Woodbury, N.Y.)·2019

    Area of Science:

    • Biochemistry
    • Pharmacology
    • Molecular Biology

    Background:

    • Calmodulin is a key calcium-binding protein involved in cellular signaling.
    • Felodipine is a dihydropyridine calcium channel antagonist.
    • Calmodulin antagonists can modulate the binding of other molecules to calmodulin.

    Purpose of the Study:

    • To investigate the binding kinetics of felodipine to calmodulin.
    • To determine the effect of calmodulin antagonists (prenylamine and R24571) on felodipine binding.
    • To elucidate the allosteric mechanisms involved in felodipine-calmodulin interactions.

    Main Methods:

    • Equilibrium dialysis
    • Fluorescence spectroscopy
    • Hill equation analysis
    • Drug titration studies

    Main Results:

    • Felodipine binding to calmodulin exhibits cooperativity with a Hill coefficient of 2.
    • Calmodulin antagonists prenylamine and R24571 significantly increase felodipine binding affinity (25-fold decrease in K0.5).
    • These antagonists act via an allosteric mechanism, enhancing affinity for felodipine at remaining binding sites.
    • Calcium dependence of felodipine binding is altered by R24571, showing increased affinity.

    Conclusions:

    • Prenylamine and R24571 act as allosteric modulators of felodipine binding to calmodulin.
    • The study proposes a model for allosterically regulated calmodulin conformers.
    • Understanding these interactions is crucial for developing drugs targeting calmodulin-dependent pathways.

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