amphotericin-b and platencin

amphotericin-b has been researched along with platencin* in 1 studies

Other Studies

1 other study(ies) available for amphotericin-b and platencin

Article	Year
Discovery of platencin, a dual FabF and FabH inhibitor with in vivo antibiotic properties. Proceedings of the National Academy of Sciences of the United States of America, 2007, May-01, Volume: 104, Issue:18 Emergence of bacterial resistance is a major issue for all classes of antibiotics; therefore, the identification of new classes is critically needed. Recently we reported the discovery of platensimycin by screening natural product extracts using a target-based whole-cell strategy with antisense silencing technology in concert with cell free biochemical validations. Continued screening efforts led to the discovery of platencin, a novel natural product that is chemically and biologically related but different from platensimycin. Platencin exhibits a broad-spectrum Gram-positive antibacterial activity through inhibition of fatty acid biosynthesis. It does not exhibit cross-resistance to key antibiotic resistant strains tested, including methicillin-resistant Staphylococcus aureus, vancomycin-intermediate S. aureus, and vancomycin-resistant Enterococci. Platencin shows potent in vivo efficacy without any observed toxicity. It targets two essential proteins, beta-ketoacyl-[acyl carrier protein (ACP)] synthase II (FabF) and III (FabH) with IC50 values of 1.95 and 3.91 microg/ml, respectively, whereas platensimycin targets only FabF (IC50 = 0.13 microg/ml) in S. aureus, 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. Topics: 3-Oxoacyl-(Acyl-Carrier-Protein) Synthase; Aminophenols; Anti-Bacterial Agents; Enzyme Inhibitors; Microbial Viability; Molecular Structure; Polycyclic Compounds	2007

Article

Year

Discovery of platencin, a dual FabF and FabH inhibitor with in vivo antibiotic properties.

Proceedings of the National Academy of Sciences of the United States of America, 2007, May-01, Volume: 104, Issue:18

Emergence of bacterial resistance is a major issue for all classes of antibiotics; therefore, the identification of new classes is critically needed. Recently we reported the discovery of platensimycin by screening natural product extracts using a target-based whole-cell strategy with antisense silencing technology in concert with cell free biochemical validations. Continued screening efforts led to the discovery of platencin, a novel natural product that is chemically and biologically related but different from platensimycin. Platencin exhibits a broad-spectrum Gram-positive antibacterial activity through inhibition of fatty acid biosynthesis. It does not exhibit cross-resistance to key antibiotic resistant strains tested, including methicillin-resistant Staphylococcus aureus, vancomycin-intermediate S. aureus, and vancomycin-resistant Enterococci. Platencin shows potent in vivo efficacy without any observed toxicity. It targets two essential proteins, beta-ketoacyl-[acyl carrier protein (ACP)] synthase II (FabF) and III (FabH) with IC50 values of 1.95 and 3.91 microg/ml, respectively, whereas platensimycin targets only FabF (IC50 = 0.13 microg/ml) in S. aureus, 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.

Topics: 3-Oxoacyl-(Acyl-Carrier-Protein) Synthase; Aminophenols; Anti-Bacterial Agents; Enzyme Inhibitors; Microbial Viability; Molecular Structure; Polycyclic Compounds

2007