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.
Publication types
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Research Support, Non-U.S. Gov't
MeSH terms
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Antineoplastic Agents / chemical synthesis*
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Antineoplastic Agents / pharmacology
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Aspergillus fumigatus / enzymology
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Biological Products / chemical synthesis
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Biological Products / chemistry
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Chitinases / antagonists & inhibitors*
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Chitinases / chemistry
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Crystallography, X-Ray
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Kinetics
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Models, Molecular
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Peptides, Cyclic / chemical synthesis*
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Peptides, Cyclic / chemistry
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Structure-Activity Relationship
Substances
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Antineoplastic Agents
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Biological Products
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Peptides, Cyclic
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argifin
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Chitinases