CJ-12,373, a novel topoisomerase II inhibitor: fermentation, isolation, structure elucidation and biological activities.
A novel isochroman carboxylic acid CJ-12,373 was isolated from Penicillium sp. CL22557. CJ-12,373 inhibits both DNA gyrase-mediated supercoiling and relaxation without the formation of a cleavage intermediate, suggesting that CJ-12,373 inhibits DNA gyrase at a stage distinct from the religation step. CJ-12,373 is not selective for procaryotic DNA gyrase as it also inhibits relaxation mediated by eukaryotic topoisomerase II. The antimicrobial potency of CJ-12,373, however, is largely attributed to its inhibition of DNA gyrase.
Inagaki
T
T
Central Research Division, Pfizer Pharmaceuticals Inc., Aichi, Japan.
Kaneda
K
K
Suzuki
Y
Y
Hirai
H
H
Nomura
E
E
Sakakibara
T
T
Yamauchi
Y
Y
Huang
L H
LH
Norcia
M
M
Wondrack
L M
LM
Sutcliffe
J A
JA
Kojima
N
N
D000900:Anti-Bacterial Agents / Q000737:chemistry / Q000302:isolation & purification / Q000494:pharmacology; D002839:Chromans / Q000737:chemistry* / Q000302:isolation & purification* / Q000494:pharmacology; D004791:Enzyme Inhibitors / Q000737:chemistry* / Q000302:isolation & purification* / Q000494:pharmacology; D004926:Escherichia coli / Q000187:drug effects / Q000201:enzymology; D005285:Fermentation; D008826:Microbial Sensitivity Tests; D015394:Molecular Structure; D010407:Penicillium; D059005:Topoisomerase II Inhibitors
D000900:Anti-Bacterial Agents; C111760:CJ 12373; D002839:Chromans; D004791:Enzyme Inhibitors; D059005:Topoisomerase II Inhibitors