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PDBsum entry 2n27
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Metal binding protein
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PDB id
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2n27
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References listed in PDB file
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Key reference
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Title
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Competitive inhibition of trpv1-Calmodulin interaction by vanilloids.
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Authors
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A.Hetényi,
L.Németh,
E.Wéber,
G.Szakonyi,
Z.Winter,
K.Jósvay,
Ã.‰.Bartus,
Z.Oláh,
T.A.Martinek.
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Ref.
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Febs Lett, 2016,
590,
2768-2775.
[DOI no: ]
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PubMed id
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Abstract
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There is enormous interest toward vanilloid agonists of the pain receptor TRPV1
in analgesic therapy, but the mechanisms of their sensory neuron-blocking
effects at high or repeated doses are still a matter of debate. Our results have
demonstrated that capsaicin and resiniferatoxin form nanomolar complexes with
calmodulin, and competitively inhibit TRPV1-calmodulin interaction. These
interactions involve the protein recognition interface of calmodulin, which is
responsible for all of the cell-regulatory calmodulin-protein interactions.
These results draw attention to a previously unknown vanilloid target, which may
contribute to the explanation of the paradoxical pain-modulating behavior of
these important pharmacons.
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