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Atpenins, potent and specific inhibitors of mitochondrial complex II (succinate-ubiquinone oxidoreductase)
TLDR
Atpenins potently and specifically inhibit the succinate-ubiquinone reductase activity of mitochondrial complex II, suggesting that atpenins may be useful tools for clarifying the biochemical and structural properties ofcomplex II, as well as for determining its physiological roles in mammalian tissues.
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Structural and Computational Analysis of the Quinone-binding Site of Complex II (Succinate-Ubiquinone Oxidoreductase)
TLDR
A mechanism for the reduction of ubiquinone during the catalytic turnover of the enzyme SQR is proposed, and two binding positions are proposed for the E. coli SQR quinone-binding site to explain these data.
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A small-molecule inhibitor of the bacterial type III secretion system protects against in vivo infection with Citrobacter rodentium
TLDR
In vivo infection study using mice clearly indicated that the administration of aurodox allowed the mice to survive a lethal dose of Citrobactor rodentium, a model bacterium for human pathogens such as EPEC, and directly demonstrated for the first time that this putative T3SS inhibitor can be applied as a novel class of anti-infective agents.
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Advances in drug discovery and biochemical studies.
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Polymyxin B identified as an inhibitor of alternative NADH dehydrogenase and malate: quinone oxidoreductase from the Gram-positive bacterium Mycobacterium smegmatis.
TLDR
Screening of the library with bacterial respiratory enzymes resulted in unprecedented findings, so it is hoped that continuing efforts could identify lead compounds for new drugs targeting to mycobacterial respiratory enzymes.
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Specificity and affinity of natural product cyclopentapeptide inhibitors against A. fumigatus, human, and bacterial chitinases.
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Spoxazomicins A–C, novel antitrypanosomal alkaloids produced by an endophytic actinomycete, Streptosporangium oxazolinicum K07-0460T
TLDR
Three novel antitrypanosomal alkaloids were isolated by silica gel column chromatography and HPLC from the culture broth of a new endophytic actinomycete species and shown to be new types of pyochelin family antibiotic.
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Potent antimalarial activities of polyether antibiotic, X-206.
TLDR
Comparison of biological activities and ion-affinities of the above antibiotics suggests that monovalent cations play an important biological role for the intracellular growth of P. falciparum in parasitized erythrocytes.
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Andrastins A-C, new protein farnesyltransferase inhibitors produced by Penicillium sp. FO-3929. I. Producing strain, fermentation, isolation, and biological activities.
New protein farnesyltransferase inhibitors, andrastins A-C, have been discovered in the cultured broth of Penicillium sp. FO-3929. Andrastins extracted from broth supernatant were purified by silica…
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Funalenone, a novel collagenase inhibitor produced by Aspergillus niger.
Funalenone, a phenalene compound that inhibits type I collagenase (MMP-1), was isolated from mycelium of Aspergillus niger FO-5904 by solvent extaction, ODS column chromatography, Sephadex LH-20…
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