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A novel telomerase template antagonist (GRN163) as a potential anticancer agent.
Optimization of the sequence, length, and bioavailability resulted in the selection of a 13-mer NPS oligonucleotide, GRN163, as a drug development candidate and it is demonstrated thatGRN163 has significant potential for additional development as an anticancer agent.
Induction of topoisomerase II-mediated DNA cleavage by the plant naphthoquinones plumbagin and shikonin
- N. Fujii, Y. Yamashita, Y. Arima, M. Nagashima, H. Nakano
- Chemistry, BiologyAntimicrobial Agents and Chemotherapy
- 1 December 1992
Plumbagin and shikonin induced a similar DNA cleavage pattern with topoisomerase II which was different from the cleavage patterns induced with other known topoisomersase II-active drugs.
K858, a novel inhibitor of mitotic kinesin Eg5 and antitumor agent, induces cell death in cancer cells.
K858 exhibited potent antitumor activity in xenograft models of cancer, and induced the accumulation of mitotic cells with monopolar spindles in tumor tissues, and was not neurotoxic in a motor coordination test in mice, representing an important compound for further investigation as a novel anticancer therapeutic.
UCH9, a new antitumor antibiotic produced by Streptomyces: I. Producing organism, fermentation, isolation and biological activities.
A microbial prescreen using Bacillus stearothermophilus NUB3620 and bacteriophage TP-68 to detect potential antitumor compounds acting on DNA or topoisomerases found that Streptomyces sp.
Belactosin A, a novel antitumor antibiotic acting on cyclin/CDK mediated cell cycle regulation, produced by Streptomyces sp.
- A. Asai, A. Hasegawa, K. Ochiai, Y. Yamashita, T. Mizukami
- Biology, ChemistryJournal of antibiotics (Tokyo. )
- 25 January 2000
The compounds which can rescue thecyclin A1-induced growth arrest might be the new antitumor drug candidates acting on the cyclin/CDK-mediated cell cycle regulation.
Induction of a heat-stable topoisomerase II-DNA cleavable complex by nonintercalative terpenoides, terpentecin and clerocidin.
It is shown that terpentecin and clerocidin induce topoisomerase II-mediated DNA cleavage in vitro with comparable potency to that of demethylepipodophyllotoxin ethylidene-beta-D-glucoside, suggesting that topoisomersase II is a cellular target for these drugs.
TELOMERASE INHIBITORS – OLIGONUCLEOTIDE PHOSPHORAMIDATES AS POTENTIAL THERAPEUTIC AGENTS
- S. Gryaznov, K. Pongracz, Y. Yamashita
- Chemistry, BiologyNucleosides, nucleotides & nucleic acids
- 31 March 2001
Various oligonucleotide N3′ → P5′ phosphoramidates, as potential telomerase inhibitors, demonstrated sequence specific and dose dependent activity with IC50 values in the sub-nM to pM concentration range.
Induction of mammalian DNA topoisomerase I mediated DNA cleavage by antitumor indolocarbazole derivatives.
- Y. Yamashita, N. Fujii, C. Murakata, T. Ashizawa, M. Okabe, H. Nakano
- Chemistry, BiologyBiochemistry
- 8 December 1992
The results indicate that KT6006 and KT6528 represent a new distinct class of mammalian DNA topoisomerase I active antitumor drugs that have different properties with respect to their interaction with DNA.
Induction of mammalian DNA topoisomerase I-mediated DNA cleavage and DNA winding by bulgarein.
Inhibitors of DNA topoisomerase I and II isolated from the Coptis rhizomes.
Results indicated that protoberberine alkaloids are a chemical family which can induce cleavable complexes with topoisomerases I and II.