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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.
A Potent Synthetic LXR Agonist Is More Effective than Cholesterol Loading at Inducing ABCA1 mRNA and Stimulating Cholesterol Efflux*
TLDR
Data show that APD is a more effective LXR agonist than endogenous oxysterols, and may therefore be useful for the prevention and treatment of atherosclerosis, especially in the context of low HDL levels.
L-696,474, a novel cytochalasin as an inhibitor of HIV-1 protease. III. Biological activity.
TLDR
A novel cytochalasin with a molecular weight of 477 and an empirical formula of C30H39NO4 inhibited HIV-1 protease activity with an IC50 of 3 microM and the mode of inhibition was competitive with respect to substrate (apparent Ki = 1 microM).
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.
Novel antinematodal and antiparasitic agents from Penicillium charlesii. I. Fermentation, isolation and biological activity.
TLDR
Paraherquamide and six novel analogs isolated from the fermentation of Penicillium charlesii displayed potent antinematodal activity against Caenorhabditis elegans.
Coniothyrione, a chlorocyclopentandienylbenzopyrone as a bacterial protein synthesis inhibitor discovered by antisense technology.
TLDR
The antisense-rpsD gene-sensitized two-plate assay led to the discovery of a novel chlorinated cyclopentandienylbenzopyrone antibiotic, coniothyrione, C14H9ClO6, isolated from Coniothyrium cerealis MF7209.
Hinnuliquinone, a C2-symmetric dimeric non-peptide fungal metabolite inhibitor of HIV-1 protease.
TLDR
Screening of microbial extracts followed by bioassay-guided isolation led to the discovery of a natural hinnuliquinone, a C(2)-symmetric bis-indolyl quinone natural product that inhibited the wild-type and a clinically resistant (A44) strain of HIV-1 protease.
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.
Nodulisporic Acid A, a Novel and Potent Insecticide from a Nodulisporium Sp. Isolation, Structure Determination, and Chemical Transformations
The potent insecticidal agent nodulisporic acid A (1a), representative of a new class of indole terpenes, was isolated from fermentations of a Nodulisporium sp. Nodulisporic acid A was active against
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