Structure based design of a ricin antidote

dc.contributor.advisorRobertus, Jon D.en
dc.contributor.committeeMemberHackert, Marvin Len
dc.creatorJasheway, Karl Richarden
dc.date.accessioned2013-02-27T17:29:08Zen
dc.date.issued2012-12en
dc.date.submittedDecember 2012en
dc.date.updated2013-02-27T17:29:09Zen
dc.descriptiontexten
dc.description.abstractRicin is a potent cytotoxin easily purified in large quantities. It presents a significant public health concern due to its potential use as a bioterrorism agent. For this reason, extensive efforts have been underway to develop antidotes against this deadly poison. The catalytic A subunit of the heterodimeric toxin has been biochemically and structurally well characterized, and is an attractive target for structure-based drug design. Aided by computer docking simulations, several ricin toxin A chain (RTA) inhibitors have been identified; the most promising leads belonging to the pterin family. To date, the most potent RTA inhibitors developed using this approach are only modest inhibitors with apparent IC50 values in the 10-4 M range, leaving significant room for improvement. This thesis discusses the development of a subset of inhibitors belonging to the pterin family in which amino acids have been utilized as building blocks. Inhibitors in this family have achieved a significant increase in potency, and have provided valuable structural information for further development.en
dc.description.departmentCellular and Molecular Biologyen
dc.format.mimetypeapplication/pdfen
dc.identifier.urihttp://hdl.handle.net/2152/19651en
dc.language.isoen_USen
dc.subjectRicinen
dc.subjectDrug designen
dc.subjectPterinen
dc.subjectToxinen
dc.subjectX-ray crystallographyen
dc.subjectProtein structureen
dc.subjectVirtual drug screeningen
dc.titleStructure based design of a ricin antidoteen
thesis.degree.departmentCellular and Molecular Biologyen
thesis.degree.disciplineCell and Molecular Biologyen
thesis.degree.grantorThe University of Texas at Austinen
thesis.degree.levelMastersen
thesis.degree.nameMaster of Artsen

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