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Title
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Drug binding by calmodulin: crystal structure of a calmodulin-trifluoperazine complex.
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Authors
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W.J.Cook,
L.J.Walter,
M.R.Walter.
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Ref.
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Biochemistry, 1994,
33,
15259-15265.
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PubMed id
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Abstract
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The crystal structure of calmodulin (CaM) bound to trifluoperazine (TFP) has
been determined and refined to a resolution of 2.45 A. Only one TFP is bound to
CaM, but that is sufficient to cause distortion of the central alpha-helix and
juxtaposition of the N- and C-terminal domains similar to that seen in
CaM-polypeptide complexes. The drug makes extensive contacts with residues in
the C-terminal domain of CaM but only a few contacts with one residue in the
N-terminal domain. The structure suggests that substrate binding to the
C-terminal domain is sufficient to cause the conformational changes in
calmodulin that lead to activation of its targets.
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