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Platensimycin is a selective FabF inhibitor with potent antibiotic properties
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.
Discovery of platencin, a dual FabF and FabH inhibitor with in vivo antibiotic properties
Platencin shows potent in vivo efficacy without any observed toxicity, emphasizing the fact that more antibiotics with novel structures and new modes of action can be discovered by using this antisense differential sensitivity whole-cell screening paradigm.
Discovery of a Small Molecule That Inhibits Cell Division by Blocking FtsZ, a Novel Therapeutic Target of Antibiotics*
Viriditoxin exhibited broad-spectrum antibacterial activity against clinically relevant Gram-positive pathogens, including methicillin-resistant Staphylococcus aureus and vancomycin-resistant Enterococci, without affecting the viability of eukaryotic cells.
Discovery and development of first in class antifungal caspofungin (CANCIDAS®)--a case study.
This paper describes a fifteen year journey from concept to clinical discovery and development of the first in class caspofungin acetate (CANCIDAS®) a parenteral antifungal agent.
A Potent Synthetic LXR Agonist Is More Effective than Cholesterol Loading at Inducing ABCA1 mRNA and Stimulating Cholesterol Efflux*
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.
Structure and chemistry of apicidins, a class of novel cyclic tetrapeptides without a terminal alpha-keto epoxide as inhibitors of histone deacetylase with potent antiprotozoal activities.
The isolation and structure elucidation of new apicidins from two Fusarium species, temperature-dependent NMR studies of apicIDin, NMR and molecular modeling based conformation of the 12-membered macrocyclic ring, and selected chemical modifications of Apicidin have been detailed in this paper.
Discovery of a potent and selective small molecule hGPR91 antagonist.