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PDBsum entry 1ptq
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Phosphotransferase
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PDB id
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1ptq
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References listed in PDB file
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Key reference
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Title
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Crystal structure of the cys2 activator-Binding domain of protein kinase c delta in complex with phorbol ester.
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Authors
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G.Zhang,
M.G.Kazanietz,
P.M.Blumberg,
J.H.Hurley.
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Ref.
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Cell, 1995,
81,
917-924.
[DOI no: ]
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PubMed id
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Abstract
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Protein kinase Cs (PKCs) are a ubiquitous family of regulatory enzymes that
associate with membranes and are activated by diacylglycerol or tumor-promoting
agonists such as phorbol esters. The structure of the second activator-binding
domain of PKC delta has been determined in complex with phorbol 13-acetate,
which binds in a groove between two pulled-apart beta strands at the tip of the
domain. The C3, C4, and C20 phorbol oxygens form hydrogen bonds with main-chain
groups whose orientation is controlled by a set of highly conserved residues.
Phorbol binding caps the groove and forms a contiguous hydrophobic surface
covering one-third of the domain, explaining how the activator promotes
insertion of PKC into membranes.
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