Antibiotics GE23077, novel inhibitors of bacterial RNA polymerase. I. Taxonomy, isolation and characterization.
GE 23077 factors A1, A2, B1 and B2 are novel antibiotics isolated from fermentation broths of an Actinomadura sp. strain. GE23077 antibiotics are cyclic peptides, which inhibit Escherichia coli RNA polymerase at nM concentrations. Both rifampicin-sensitive and rifampicin-resistant polymerases are inhibited, whereas E. coli DNA polymerase and wheat germ RNA polymerase are substantially not affected. In spite of the potent activity on the enzyme, the antibiotics generally show poor activity against whole cell bacteria. The spectrum of activity is restricted to Moraxella catarrhalis, including clinical isolates, with partial activity against Neisseria gonorrhoeae and Mycobacterium smegmatis.
Ciciliato
Ismaela
I
Vicuron Pharmaceuticals, Via R. Lepetit 34, 21040 Gerenzano, Varese, Italy.
Corti
Emiliana
E
Sarubbi
Edoardo
E
Stefanelli
Stefania
S
Gastaldo
Luciano
L
Montanini
Nicoletta
N
Kurz
Michael
M
Losi
Daniele
D
Marinelli
Flavia
F
Selva
Enrico
E
D000900:Anti-Bacterial Agents / Q000145:classification / Q000302:isolation & purification* / Q000494:pharmacology; D001419:Bacteria / Q000187:drug effects / Q000201:enzymology; D002851:Chromatography, High Pressure Liquid; D012321:DNA-Directed RNA Polymerases / Q000037:antagonists & inhibitors*; D004791:Enzyme Inhibitors / Q000145:classification / Q000302:isolation & purification* / Q000494:pharmacology; D004926:Escherichia coli / Q000187:drug effects / Q000201:enzymology; D005285:Fermentation; D019384:Nucleic Acid Synthesis Inhibitors; D013329:Structure-Activity Relationship
D000900:Anti-Bacterial Agents; D004791:Enzyme Inhibitors; D019384:Nucleic Acid Synthesis Inhibitors; D012321:DNA-Directed RNA Polymerases