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An efficient synthesis of argifin: a natural product chitinase inhibitor with chemotherapeutic potential
Authors:Dixon Mark J  Andersen Ole A  van Aalten Daan M F  Eggleston Ian M
Institution:Division of Biological Chemistry and Molecular Microbiology, School of Life Sciences, University of Dundee, Dundee DD1 5EH, UK.
Abstract:The first synthesis of the cyclopentapeptide family 18 chitinase inhibitor argifin has been achieved by a combination of solid phase and solution chemistry. Synthetic argifin is a nanomolar inhibitor of chitinase B1 from Aspergillus fumigatus and the high-resolution X-ray structure of the synthesized material in complex with the same enzyme is identical to that previously obtained for the natural product.
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