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Chemical Compound Review

CHEMBL96510     1-cyclopropyl-6,8-difluoro-7- (4...

Synonyms: AG-D-74273, ACMC-20mw5z, SureCN13576362, CHEBI:254670, AC1L3OOK, ...
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High impact information on CP 115953

  • Introduction of the Ser741-->Trp mutation into yeast TOP2 confers resistance to 6,8-difluoro-7-(4'-hydroxyphenyl)-1-cyclopropyl- 4-quinolone-3-carboxylic acid (CP-115,953), a fluoroquinolone with substantial activity against eukaryotic topoisomerase II, whereas changing Ser741 to either Leu or Ala does not change sensitivity to quinolones [1].
  • A mutant yeast type II topoisomerase was generated by in vitro mutagenesis followed by selection in vivo for resistance to the quinolone CP-115,953 [2].
  • Cytotoxicity of quinolones toward eukaryotic cells. Identification of topoisomerase II as the primary cellular target for the quinolone CP-115,953 in yeast [3].
  • CP-67,804 was nearly as potent an enhancer as etoposide, while CP-115,953 was approximately 2 times more potent than this topoisomerase II-targeted antineoplastic drug [4].
  • Although quinolone cross-resistance was less pronounced than observed for etoposide (approximately 12-fold), it indicates that topoisomerase II is a physiological target for CP-67,804 and CP-115,953 in mammalian cells [4].

Biological context of CP 115953


Anatomical context of CP 115953

  • CP-115,953 stimulates cytokine production by lymphocytes [5].
  • Therefore, CP-115,953 and a series of related quinolones were examined for their activity against calf thymus topoisomerase II and cultured mammalian cells [6].

Associations of CP 115953 with other chemical compounds


Gene context of CP 115953


  1. A mutation in yeast TOP2 homologous to a quinolone-resistant mutation in bacteria. Mutation of the amino acid homologous to Ser83 of Escherichia coli gyrA alters sensitivity to eukaryotic topoisomerase inhibitors. Hsiung, Y., Elsea, S.H., Osheroff, N., Nitiss, J.L. J. Biol. Chem. (1995) [Pubmed]
  2. A yeast type II topoisomerase selected for resistance to quinolones. Mutation of histidine 1012 to tyrosine confers resistance to nonintercalative drugs but hypersensitivity to ellipticine. Elsea, S.H., Hsiung, Y., Nitiss, J.L., Osheroff, N. J. Biol. Chem. (1995) [Pubmed]
  3. Cytotoxicity of quinolones toward eukaryotic cells. Identification of topoisomerase II as the primary cellular target for the quinolone CP-115,953 in yeast. Elsea, S.H., Osheroff, N., Nitiss, J.L. J. Biol. Chem. (1992) [Pubmed]
  4. Effects of quinolone derivatives on eukaryotic topoisomerase II. A novel mechanism for enhancement of enzyme-mediated DNA cleavage. Robinson, M.J., Martin, B.A., Gootz, T.D., McGuirk, P.R., Moynihan, M., Sutcliffe, J.A., Osheroff, N. J. Biol. Chem. (1991) [Pubmed]
  5. CP-115,953 stimulates cytokine production by lymphocytes. Riesbeck, K., Forsgren, A. Antimicrob. Agents Chemother. (1995) [Pubmed]
  6. Drug features that contribute to the activity of quinolones against mammalian topoisomerase II and cultured cells: correlation between enhancement of enzyme-mediated DNA cleavage in vitro and cytotoxic potential. Elsea, S.H., McGuirk, P.R., Gootz, T.D., Moynihan, M., Osheroff, N. Antimicrob. Agents Chemother. (1993) [Pubmed]
  7. Quinolones share a common interaction domain on topoisomerase II with other DNA cleavage-enhancing antineoplastic drugs. Elsea, S.H., Westergaard, M., Burden, D.A., Lomenick, J.P., Osheroff, N. Biochemistry (1997) [Pubmed]
  8. Effects of novel fluoroquinolones on the catalytic activities of eukaryotic topoisomerase II: Influence of the C-8 fluorine group. Robinson, M.J., Martin, B.A., Gootz, T.D., McGuirk, P.R., Osheroff, N. Antimicrob. Agents Chemother. (1992) [Pubmed]
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