Journal
BIOORGANIC & MEDICINAL CHEMISTRY
Volume 16, Issue 24, Pages 10345-10355Publisher
PERGAMON-ELSEVIER SCIENCE LTD
DOI: 10.1016/j.bmc.2008.10.030
Keywords
Crocacin; Respiration; Inhibitor; Fungicide; Modeling
Funding
- NIDDK NIH HHS [R01 DK044842, R01 DK044842-14] Funding Source: Medline
- NIGMS NIH HHS [R01 GM038237, R01 GM038237-22] Funding Source: Medline
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Extensive molecular modeling based on crystallographic data was used to aid the design of synthetic analogues of the fungicidal naturally occurring respiration inhibitors crocacins A and D, and an inhibitor binding model to the mammalian cytochrome bc(1) complex was constructed. Simplified analogues were made which showed high activity in a mitochondrial beef heart respiration assay, and which were also active against certain plant pathogens in glasshouse tests. A crystal structure was obtained of an analogue of crocacin D bound to the chicken heart cytochrome bc(1) complex, which validated the binding model and which confirmed that the crocacins are a new class of inhibitor of the cytochrome bc(1) complex. (C) 2008 Elsevier Ltd. All rights reserved.
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