An efficient synthesis of argifin: A natural product chitinase inhibitor with chemotherapeutic potential
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 synthesize...
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Veröffentlicht in: | Bioorganic & medicinal chemistry letters 2005-11, Vol.15 (21), p.4717-4721 |
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creator | Dixon, Mark J. Andersen, Ole A. van Aalten, Daan M.F. Eggleston, Ian M. |
description | 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. |
doi_str_mv | 10.1016/j.bmcl.2005.07.068 |
format | Article |
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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.</description><subject>Analytical, structural and metabolic biochemistry</subject><subject>Antineoplastic Agents - chemical synthesis</subject><subject>Antineoplastic Agents - pharmacology</subject><subject>Aspergillus fumigatus - enzymology</subject><subject>Biological and medical sciences</subject><subject>Biological Products - chemical synthesis</subject><subject>Biological Products - chemistry</subject><subject>Chitinase inhibitor</subject><subject>Chitinases - antagonists & inhibitors</subject><subject>Chitinases - chemistry</subject><subject>Crystallography, X-Ray</subject><subject>Cyclic peptide</subject><subject>Enzymes and enzyme inhibitors</subject><subject>Fundamental and applied biological sciences. Psychology</subject><subject>Hydrolases</subject><subject>Kinetics</subject><subject>Medical sciences</subject><subject>Miscellaneous</subject><subject>Models, Molecular</subject><subject>Natural product</subject><subject>Peptides, Cyclic - chemical synthesis</subject><subject>Peptides, Cyclic - chemistry</subject><subject>Pharmacology. 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source | MEDLINE; Elsevier ScienceDirect Journals |
subjects | Analytical, structural and metabolic biochemistry Antineoplastic Agents - chemical synthesis Antineoplastic Agents - pharmacology Aspergillus fumigatus - enzymology Biological and medical sciences Biological Products - chemical synthesis Biological Products - chemistry Chitinase inhibitor Chitinases - antagonists & inhibitors Chitinases - chemistry Crystallography, X-Ray Cyclic peptide Enzymes and enzyme inhibitors Fundamental and applied biological sciences. Psychology Hydrolases Kinetics Medical sciences Miscellaneous Models, Molecular Natural product Peptides, Cyclic - chemical synthesis Peptides, Cyclic - chemistry Pharmacology. Drug treatments Solid phase synthesis Structure-Activity Relationship |
title | An efficient synthesis of argifin: A natural product chitinase inhibitor with chemotherapeutic potential |
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