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Baulamycins A and B, Broad-Spectrum Antibiotics Identified as Inhibitors of Siderophore Biosynthesis in Staphylococcus aureus and Bacillus anthracis
(2014)
Siderophores are high-affinity iron chelators produced by microorganisms and frequently contribute to the virulence of human pathogens. Targeted inhibition of the biosynthesis of siderophores staphyloferrin B of Staphylococcus ...
Adipostatins E-J, new potent antimicrobials identified as inhibitors of coenzyme-A biosynthesis
(2020-01)
Phosphopantetheine is a key structural element in biological acyl transfer reactions found embedded within coenzyme A (CoA). Phosphopantothenoylcysteine synthetase (PPCS) is responsible for installing a cysteamine group ...
The Combined Use of Alphavirus Replicons and Pseudoinfectious Particles for the Discovery of Antivirals Derived from Natural Products
(2015)
Alphaviruses are a prominent class of reemergent pathogens due to their globally expanding ranges, potential for lethality, and possible use as bioweapons. The absence of effective treatments for alphaviruses highlights ...
Identification of Protein Kinase C Activation as a Novel Mechanism for RGS2 Protein Upregulation through Phenotypic Screening of Natural Product Extracts
(2014)
Biochemical high-throughput screening is widely used in drug discovery, using a variety of small molecule libraries. However, broader screening strategies may be more beneficial to identify novel biologic mechanisms. In ...
Titration-Based Screening for Evaluation of Natural Product Extracts: Identification of an Aspulvinone Family of Luciferase Inhibitors
(2011)
The chemical diversity of nature has tremendous potential for the discovery of molecular probes and medicinal agents. However, sensitivity of HTS assays to interfering components of crude extracts derived from plants, and ...
Sekikaic Acid and Lobaric Acid Target a Dynamic Interface of the Coactivator CBP/p300
(2012-10-08)
Although there have been recent notable successes in thediscovery of ligands that target stable, high-affinity protein-protein interactions (PPIs), the transient and moderateaffinity PPIs that underpin many fundamental ...