title: Structural biology and structure-based inhibitor design of cholera toxin and heat-labile enterotoxin.
abstract: Structural biology studies on cholera toxin and the closely related heat-labile enterotoxin from enterotoxigenic Escherichia coli over the past decade have shed light on the mechanism of toxin action at molecular and atomic levels. Also, components of the extracellular protein secretion apparatus that translocate the toxins across the outer membrane are being investigated. At the same time, structure-based design has led to various classes of compounds targeting different toxin sites, including highly potent multivalent inhibitors that block the toxin receptor-binding process.
authors.affiliation: Department of Biochemistry, Biomolecular Structure Center, University of Washington, Box 357742, Seattle WA 98195, USA.
authors.forename: Erkang
authors.initials: E
authors.lastname: Fan
authors.forename: Claire J
authors.initials: CJ
authors.lastname: O'Neal
authors.forename: Daniel D
authors.initials: DD
authors.lastname: Mitchell
authors.forename: Mark A
authors.initials: MA
authors.lastname: Robien
authors.forename: Zhongsheng
authors.initials: Z
authors.lastname: Zhang
authors.forename: Jason C
authors.initials: JC
authors.lastname: Pickens
authors.forename: Xiao-Jian
authors.initials: XJ
authors.lastname: Tan
authors.forename: Konstantin
authors.initials: K
authors.lastname: Korotkov
authors.forename: Claudia
authors.initials: C
authors.lastname: Roach
authors.forename: Brian
authors.initials: B
authors.lastname: Krumm
authors.forename: Christophe L M J
authors.initials: CL
authors.lastname: Verlinde
authors.forename: Ethan A
authors.initials: EA
authors.lastname: Merritt
authors.forename: Wim G J
authors.initials: WG
authors.lastname: Hol
mesh_terms: D001427:Bacterial Toxins / Q000037:antagonists & inhibitors / Q000737:chemistry* / Q000378:metabolism; D002772:Cholera Toxin / Q000037:antagonists & inhibitors / Q000737:chemistry* / Q000378:metabolism; D018360:Crystallography, X-Ray; D004768:Enterotoxins / Q000037:antagonists & inhibitors / Q000737:chemistry* / Q000378:metabolism; D004926:Escherichia coli / Q000378:metabolism*; D029968:Escherichia coli Proteins / Q000037:antagonists & inhibitors / Q000737:chemistry* / Q000378:metabolism; D006801:Humans; D008958:Models, Molecular; D013329:Structure-Activity Relationship; D014734:Vibrio cholerae / Q000378:metabolism*
chemical_list: D001427:Bacterial Toxins; D004768:Enterotoxins; D029968:Escherichia coli Proteins; D002772:Cholera Toxin; C027538:heat-labile enterotoxin, E coli