article · Drugs of the Future · 2003

Helicase-primase inhibitors

Cited by 8Abstract and details only

Abstract

The protein family of helicases separate or unwind duplex nucleic acids such as oligonucleotides, RNA or DNA into single strands. This enzymatic activity is essential for metabolic processes of DNA and RNA replication, transcription etc. and are often associated in enzyme complexes. To multiply, many pathogens encode their own helicase and/or primase to synthesize DNA. Inhibition of this enzymatic activity abrogates microbial propagation and can lead to the development of potent drugs for treating and curing infection. Recently, helicase-primase inhibitors were reported for the treatment of herpes simplex disease. Almost 25 years after the launch of the milestone antiherpes drug aciclovir (20virax), these drug candidates represent the first compound class which outperforms the only available nucleosidic inhibitors of the herpes TK/DNA-polymerase with respect to all predinical pharmacologicai parameters. The helicase-primase enzyme complex appears to be the Achilles heel of herpes simplex viruses and is a prime target of antiinfective drug discovery. The antibiotic ciprofloxacin inhibits the bacterial topoisomerase II (DNA-gyrase) and IV and thus interferes with supercoiling of DNA. Drugs that inhibit supercoiling or unwinding of DNA seem to be the most effective antimicrobial agents. The mechanism of action of these drugs is based not only on the inhibition of a target but also on a mode of action that triggers subsequent molecular events. cascades and pathways which prevent propagation and even survival of the pathogen.

Cite this paper

APA 7

Kleymann, G. (2003). Helicase-primase inhibitors. Drugs of the Future, 28(3), 0257. https://doi.org/10.1358/dof.2003.028.03.856930

MLA 9

Kleymann, Gerald. “Helicase-primase inhibitors.” Drugs of the Future, vol. 28, no. 3, 2003, p. 0257, https://doi.org/10.1358/dof.2003.028.03.856930.

Chicago

Kleymann, Gerald. 2003. “Helicase-primase inhibitors.” Drugs of the Future 28 (3): 0257. https://doi.org/10.1358/dof.2003.028.03.856930.

Harvard

Kleymann, G. (2003) ‘Helicase-primase inhibitors’, Drugs of the Future, 28(3), p. 0257. Available at: https://doi.org/10.1358/dof.2003.028.03.856930.

BibTeX

@article{kleymann2003helicase,
  title = {{Helicase-primase inhibitors}},
  author = {Kleymann, Gerald},
  journal = {Drugs of the Future},
  volume = {28},
  number = {3},
  pages = {0257},
  year = {2003},
  doi = {10.1358/dof.2003.028.03.856930}
}

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