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Platensimycin is a selective FabF inhibitor with potent antibiotic properties
TLDR
Platensimycin demonstrates strong, broad-spectrum Gram-positive antibacterial activity by selectively inhibiting cellular lipid biosynthesis through the selective targeting of β-ketoacyl-(acyl-carrier-protein (ACP) in the synthetic pathway of fatty acids.
Isolation, structure, and absolute stereochemistry of platensimycin, a broad spectrum antibiotic discovered using an antisense differential sensitivity strategy.
TLDR
It was determined that potential reactivity of the enone moiety does not play a key role in the biological activity of platensimycin and cyclohexenone ring conformation renders for the stronger binding interaction with the enzyme.
Isolation, structure, and antibacterial activity of philipimycin, a thiazolyl peptide discovered from Actinoplanes philippinensis MA7347.
TLDR
A highly specific assay with a pair of thiazomycin sensitive and resistant strains of Staphylococcus aureus led to the discovery of philipimycin, a new thiazolyl peptide glycoside, which showed strong antibacterial activities against gram-positive bacteria including MRSA.
Discovery of okilactomycin and congeners from Streptomyces scabrisporus by antisense differential sensitivity assay targeting ribosomal protein S4
TLDR
Screening of microbial extracts using antisense-sensitized rpsD Staphylococcus aureus strain led to isolation of okilactomycin and four new congeners from Streptomyces scabrisporus, and all compounds showed a slight preferential inhibition of RNA synthesis over DNA and protein synthesis.
Discovery of FabH/FabF Inhibitors from Natural Products
TLDR
The mechanism of decreased target protein production by expression of antisense RNA was investigated using Northern blotting and revealed that the antisenseRNA acts posttranscriptionally by targeting mRNA, leading to 5′ mRNA degradation.
Improved chiral SFC screening for analytical method development.
TLDR
The greatly improved gradient dwell volume and liquid flow control of the new instrument in combination with the use of shorter columns containing smaller stationary phase particles affords chiral SFC method development that is faster and more universal than previous systems.
Cyclic colisporifungin and linear cavinafungins, antifungal lipopeptides isolated from Colispora cavincola.
TLDR
The cyclic peptide colisporifungin displayed a strong potentiation of the growth inhibitory effect of caspofungin against Aspergillus fumigatus and, to a lesser extent, against Candida albicans.
Highly substituted terphenyls as inhibitors of parasite cGMP-dependent protein kinase activity.
TLDR
A library of natural product extracts was screened for inhibitors of parasite PKG for the discovery of anticoccidial leads and three new terphenyls were isolated using bioassay-guided fractionation of the microbial extract of a Phoma sp.
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