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J Antibiot (Tokyo) ; 63(2): 77-82, 2010 Feb.
Article in English | MEDLINE | ID: mdl-20057513

ABSTRACT

A new ryanodine-binding inhibitor, verticilide, was isolated from the cultured broth of a fungus, Verticillium sp. FKI-1033. It is a 24-membered ring cyclic depsipeptide, its structure being elucidated as cyclo[(2R)-2-hydroxyheptanoyl-N-methyl- L-alanyl](4). Verticilide inhibited ryanodine binding to ryanodine receptors in the cockroach at an IC(50) value of 4.2 microM, whereas inhibition against mouse ryanodine receptors was weak (IC(50)=53.9 microM).


Subject(s)
Depsipeptides/metabolism , Depsipeptides/pharmacology , Ryanodine Receptor Calcium Release Channel/metabolism , Ryanodine/antagonists & inhibitors , Verticillium/metabolism , Animals , Cell Membrane/metabolism , Cockroaches , Depsipeptides/chemistry , Mice , Molecular Biology , Muscle Fibers, Skeletal/metabolism , Protein Binding , Structure-Activity Relationship
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