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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 ...
Discovery of cahuitamycins as biofilm inhibitors derived from a convergent biosynthetic pathway
(2016-02-16)
Pathogenic microorganisms often have the ability to attach to a surface, building a complex matrix where they colonize to form a biofilm. This cellular superstructure can display increased resistance to antibiotics and ...
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 ...
Novel Lobophorins Inhibit Oral Cancer Cell Growth and Induce Atf4- and Chop-Dependent Cell Death in Murine Fibroblasts
(2015-07-06)
As part of the International Cooperative Biodiversity Groups (ICBG) Program, we were interested in identifying biologically active unfolded protein response (UPR) inducing compounds from marine microorganisms isolated from ...
Discovery of nicoyamycin A, an inhibitor of uropathogenic Escherichia coli growth in low iron environments
(2017)
High-throughput screening and activity-guided purification identified nicoyamycin A, a natural product comprised of an uncommon 3-methyl-1,4-dioxane ring incorporated into a desferrioxamine-like backbone via a spiroaminal ...
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 ...
Actinoramide A Identified as a Potent Antimalarial from Titration-Based Screening of Marine Natural Product Extracts
(2015)
Methods to identify the bioactive diversity within natural product extracts (NPEs) continue to evolve. NPEs constitute complex mixtures of chemical substances varying in structure, composition, and abundance. NPEs can ...
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 ...