title: Crystal structure of annexin V with its ligand K-201 as a calcium channel activity inhibitor.
abstract: The crystal structure of recombinant human annexin V complexed with K-201, an inhibitor of the calcium ion channel activity of annexin V, was solved at 3.0 A by molecular replacement including the apo and high-calcium forms. K-201 was bound at the hinge region cavity formed by the N-terminal strand and domains II, III and IV, at the side opposite the calcium and membrane-binding surface, in an L-shaped conformation. Based on the complex and other annexin structures, K-201 is proposed to restrain the hinge movement of annexin V in an allosteric manner, resulting in the inhibition of calcium movement across the annexin V molecule.
authors.affiliation: Department of Cardiology, Tokyo Women's Medical College, Japan.
authors.forename: N
authors.initials: N
authors.lastname: Kaneko
authors.forename: H
authors.initials: H
authors.lastname: Ago
authors.forename: R
authors.initials: R
authors.lastname: Matsuda
authors.forename: E
authors.initials: E
authors.lastname: Inagaki
authors.forename: M
authors.initials: M
authors.lastname: Miyano
mesh_terms: D017304:Annexin A5 / Q000737:chemistry* / Q000235:genetics / Q000378:metabolism; D002121:Calcium Channel Blockers / Q000737:chemistry*; D015220:Calcium Channels / Q000187:drug effects*; D018360:Crystallography, X-Ray; D006801:Humans; D008024:Ligands; D008958:Models, Molecular; D011485:Protein Binding; D011994:Recombinant Proteins / Q000737:chemistry; D013050:Spectrometry, Fluorescence; D013841:Thiazepines / Q000737:chemistry* / Q000378:metabolism
chemical_list: D017304:Annexin A5; D002121:Calcium Channel Blockers; D015220:Calcium Channels; D008024:Ligands; D011994:Recombinant Proteins; D013841:Thiazepines; C109183:K201 compound