ArticleAntimicrobial agents and chemotherapy1994
Selective inhibition of topoisomerases from Pneumocystis carinii compared with that of topoisomerases from mammalian cells.
Article in Antimicrobial agents and chemotherapy, 1994. The graph could read no effect estimate from its abstract, so it casts no vote on the map. Cited by 17 papers.
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Who cites it
17 citing papers in PubMed, 73 citations in OpenAlex.
- Alkanediamide-Linked Bisbenzamidines Are Promising Antiparasitic Agents.Pharmaceuticals (Basel, Switzerland) · 2016Article
- Anticancer, antioxidant activities, and DNA affinity of novel monocationic bithiophenes and analogues.Drug design, development and therapy · 2014Article
- Dicationic phenyl-2,2'-bichalcophenes and analogues as antiprotozoal agents.Bioorganic & medicinal chemistry · 2011Article
- Experimental Chemotherapy for Chagas Disease: A Morphological, Biochemical, and Proteomic Overview of Potential Trypanosoma cruzi Targets of Amidines Derivatives and Naphthoquinones.Molecular biology international · 2011Article
- Screening of Potential anti-Trypanosoma cruzi Candidates: In Vitro and In Vivo Studies.The open medicinal chemistry journal · 2011Article
- Synthesis and activity of azaterphenyl diamidines against Trypanosoma brucei rhodesiense and Plasmodium falciparum.Bioorganic & medicinal chemistry · 2009Article
- Novel linear triaryl guanidines, N-substituted guanidines and potential prodrugs as antiprotozoal agents.European journal of medicinal chemistry · 2008Article
- Molecular characterization of recombinant Pneumocystis carinii topoisomerase I: differential interactions with human topoisomerase I poisons and pentamidine.Antimicrobial agents and chemotherapy · 2002Article
- Antifungal activity of eupolauridine and its action on DNA topoisomerases.Antimicrobial agents and chemotherapy · 2002Article
- Pentamidine inhibition of group I intron splicing in Candida albicans correlates with growth inhibition.Antimicrobial agents and chemotherapy · 2000Article
- Topoisomerase I is essential in Cryptococcus neoformans: role In pathobiology and as an antifungal target.Genetics · 1999Article
- Structure-in vitro activity relationships of pentamidine analogues and dication-substituted bis-benzimidazoles as new antifungal agents.Antimicrobial agents and chemotherapy · 1998Article
- Treatment of infection due to Pneumocystis carinii.Antimicrobial agents and chemotherapy · 1998Review
- Effectiveness of quinolone antibiotics in modulating the effects of antifungal drugs.Antimicrobial agents and chemotherapy · 1997Article
- Antifungal agents: chemotherapeutic targets and immunologic strategies.Antimicrobial agents and chemotherapy · 1996Review
- Identification of the aminocatechol A-3253 as an in vitro poison of DNA topoisomerase I from Candida albicans.Antimicrobial agents and chemotherapy · 1995Article
- Synthesis of dicationic diarylpyridines as nucleic-acid binding agents.European journal of medicinal chemistry · 1995Article
Corrections and comments
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Authors and funding
4 authors at 1 institution in 1 country.
Funding
Abstract
Type I and II topoisomerase activities were partially purified from Pneumocystis carinii. The catalytic (strand-passing) activities of both enzymes were selectively inhibited by members of a series of dicationic-substituted bis-benzimidazoles compared with those of topoisomerases of mammalian (calf thymus) origin. The most active inhibitors of the parasite enzymes were also highly effective in an in vivo animal model of P. carinii pneumonia. Selected dicationic-substituted bis-benzimidazoles also strongly inhibited the induction of the topoisomerase I- and II-mediated cleavable complex, suggesting that the biologically active DNA minor groove-binding molecules inhibit the enzyme-DNA binding step of the topoisomerase reaction sequence. The apparent selectivities for the parasite enzymes and the low levels of toxicity to mammalian cells for the biologically active bis-benzimidazoles suggest that these compounds hold promise as effective therapeutic agents in the treatment of a life-threatening AIDS-related disease, P. carinii pneumonia.
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Read under generation 80e0d062 · epoch 390. Bibliography from PubMed, PubMed Central and OpenAlex; grants from NIH RePORTER; trial links from ClinicalTrials.gov; estimates, votes and beliefs from the OpenQuestion graph.