Thiophene antibacterials that allosterically stabilize DNA-cleavage complexes with DNA gyrase
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منابع مشابه
Thiophene antibacterials that allosterically stabilize DNA-cleavage complexes with DNA gyrase.
A paucity of novel acting antibacterials is in development to treat the rising threat of antimicrobial resistance, particularly in Gram-negative hospital pathogens, which has led to renewed efforts in antibiotic drug discovery. Fluoroquinolones are broad-spectrum antibacterials that target DNA gyrase by stabilizing DNA-cleavage complexes, but their clinical utility has been compromised by resis...
متن کاملInteraction between DNA gyrase and its cleavage site on DNA.
DNA gyrase negatively supercoils DNA. When the requisite breaking and resealing of the DNA are uncoupled by gyrase inhibitors, the DNA becomes cleaved at specific sites. ATP, the cofactor for supercoiling, changes the sites of DNA cleavage. The mechanism of this effect was studied at sites in ColEl and @X174 DNA at which ATP strikingly enhanced cleavage. The following results showed that this i...
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Escherichia coli DNA gyrase contains a 1:1 ratio of protomers coded by the genes gyrA and gyrB. This along with previous results shows that the enzyme has two copies of each protomer and thus a molecular weight of 400,000. Abortion of the gyrase reaction results in double-strand breakage of the DNA and covalent attachment of both gyrA protomers to the 5'-cut ends. We conclude that the gyrA prot...
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Few novel cobalt(II) and copper(II) complexes [M(fmp)3]Cl2, [M(fmp)(bpy)2]Cl2,[M(fmp)(phen)2]Cl2 and [M(fmp)(phen)(bpy)]Cl2 (fmp = 3-furan-2-ylmethylene-pentane-2,4-dione, phen = 1,10-phenanthroline, bpy = 2,2'-bipyridine) have been synthesized andcharacterized by elemental analyses, molar conductance, magnetic susceptibility measurements,IR, electronic, EPR, mass spectra and cyclic voltammetri...
متن کاملArchaebacterial reverse gyrase cleavage-site specificity is similar to that of eubacterial DNA topoisomerases I.
ATP-dependent type I topoisomerases from extremely thermophilic archaebacteria--reverse gyrases--drive positive supercoiling of DNA. We showed that reverse gyrase from Desulfurococcus amylolyticus breaks the DNA at specific sites and covalently binds to the 5' end. In 30 out of 31 sites located in pBR322 DNA fragments, cleavage occurs at the sequence 5'---CNNN/---(N is any base). The same rule ...
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ژورنال
عنوان ژورنال: Proceedings of the National Academy of Sciences
سال: 2017
ISSN: 0027-8424,1091-6490
DOI: 10.1073/pnas.1700721114