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  • clinically
  • Many clinically approved antibacterial and anticancer agents target DNA topoisomerases. (grantome.com)
  • While the community has lacked pure and stable malarial topoisomerases to work with, there are intriguing hints from preliminary data that clinically-approved antimalarials, such as pyronaridine, may inhibit malaria topoisomerases. (grantome.com)
  • Previously, the investigator, in his own laboratory and as a part of larger drug discovery teams, has helped understand clinically useful antimalarial drugs, identified new drug targets, and synthesized nanomolar level inhibitors with appropriate pharmaceutical properties. (grantome.com)
  • PARP
  • The whole range of pathological processes, from vascular disease and neoplasia to central nervous system malformations and infectious diseases (with many more besides), PARP inhibitor are summarized elegantly and succinctly in just over 260 pages. (topoisomerasesignaling.com)
  • Synthetic lethality has utility for purposes of molecular targeted cancer therapy, with the first example of a molecular targeted therapeutic exploiting a synthetic lethal exposed by an inactivated tumor suppressor gene (BRCA1 and 2) receiving FDA approval in 2016 (PARP inhibitor). (wikipedia.org)
  • cell cycle
  • It is thought that topoisomerase inhibitors block the ligation step of the cell cycle, generating single and double stranded breaks that harm the integrity of the genome. (wikipedia.org)
  • A variety of parameters in these lines were analyzed to elucidate mechanisms of resistance including S phase, doubling time, expression and activity of topoisomerase I and II, expression of mdr-1, p53 status, cell cycle arrest, level of apoptosis, and expression of the apoptotic proteins Bcl-2 and Bax. (duke.edu)
  • analogues
  • We compared the mode of topoisomerase II ATPase inhibition induced by NSC35866 with that of 12 other substituted purine analogues of different chemical classes. (aacrjournals.org)
  • In contrast, NSC35866 as well as two O 6 -substituted guanine analogues, O 6 -benzylguanine and NU2058, could inhibit topoisomerase II ATPase activity in the presence of DTT, indicating that they have a different mechanism of inhibition. (aacrjournals.org)
  • strands
  • A bacterial DNA topoisomerase II that catalyzes ATP-dependent breakage of both strands of DNA, passage of the unbroken strands through the breaks, and rejoining of the broken strands. (bioportfolio.com)