Structural biology and structure-based inhibitor design of cholera toxin and heat-labile enterotoxin

Erkang Fan, Claire J. O'Neal, Daniel D. Mitchell, Mark A. Robien, Zhongsheng Zhang, Jason C. Pickens, Xiao Jian Tan, Konstantin Korotkov, Claudia Roach, Brian Krumm, Christophe L.M.J. Verlinde, Ethan A. Merritt, Wim G.J. Hol

Research output: Contribution to journalReview articlepeer-review

42 Scopus citations


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.

Original languageEnglish
Pages (from-to)217-223
Number of pages7
JournalInternational Journal of Medical Microbiology
Issue number4
StatePublished - Oct 2004

Bibliographical note

Funding Information:
We thank the National Institutes of Health for financial support of our work (AI44954 to E. Fan; GM54618 to C. Verlinde; and AI34501 to W. Hol). C. O’Neal is a Howard Hughes Medical Institute predoctoral fellow. We are grateful to current and past members of our laboratories who have made contribution to the work described here, particularly in structural biology: Titia Sixma, Focco van den Akker, Ingeborg Feil, Bianca Nerenberg, Misol Ahn, Jan Abendroth, Steve Sarfaty, Stewart Turley, and Francis Athappilly; in inhibitor design: Wendy Sanderson; and in chemical synthesis: Zhen Hou, Feng Hong, Ajit Ghosh, Zhenfa Zhang and Jiyun Liu. We also like to thank our numerous collaborators including: Bernard Witholt, Rino Rappuoli, Joseph Martial, Randall Holmes, Michael Jobling, Timothy Hirst, Maria Sandkvist and Michael Bagdasarian.


  • Cholera toxin
  • Heat-labile enterotoxin
  • Multivalent inhibitor
  • Structure-based drug design
  • Type II secretion system

ASJC Scopus subject areas

  • Microbiology
  • Microbiology (medical)
  • Infectious Diseases


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