In a sense, cancer chemotherapy is similar to antibacterial chemotherapy. The main target for both chemotherapies is on DNA and its precursors. Whenever anticancer drugs exhibit its activity on cancer cells, damage or metabolic abnormality of DNA is usually accompanied. Among various anticancer drugs, the main cellular target of alkylating agents or anticancer antibiotics is DNA strand, and many of newly introduced anticancer drugs exert effect on DNA strand or DNA synthesis. The mechanism of action of quinocarmycin, KT 6149, which is a derivative of mitomycin C, YM534, which shows thrombocyte agglutination activity, and MCNU, a nitrosourea, were studied for their antitumor action and damage to DNA strand. It was found that there was a close relationship between anticancer effect and single strand scission of DNA in all the agents tested.

01 Dec 1989·The science reports of the research institutes, Tohoku University. Ser. C, Medicine. Tohoku Daigaku

Damage to DNA strand and the effects of anticancer drugs.

Article

Author: Ishikawa, A ; Wakui, A ; Kanamaru, R ; Shibata, H ; Konishi, Y ; Ishioka, C

Cancer chemotherapy is, in a sense, similar to the treatment of infectious disease with antibiotics. The main mechanism of action is on DNA and its precursor, and in the process that anticancer drugs exert the effect on cancer cells, the cells always have abnormal metabolism or destruction of DNA. The main cellular target of most alkylating agents, or anticancer antibiotics is DNA, however, among the anticancer drug newly synthesized, there are some compounds which exert the action on DNA. Quinocarmycin, KT6149, which is a derivative of MMC, YM534, which possesses a platelet agglutinating activity, and MCNU, a nitrosourea compound were studied on the anticancer activity and on damage to DNA strand, and it was found that the lethal effect was deeply concerned with single strand scission of DNA.

01 Aug 1989·Anti-cancer drug design

Potentiation of vincristine and actinomycin D by a new synthetic imidazole anti-tumor agent YM534 active against human cancer cells and multidrug-resistant cells.

Article

Author: Okamura, K ; Mori, T ; Hamanaka, R ; Kuwano, M ; Watanabe, Y ; Kohno, K ; Sato, S

Ethyl 6-p-5-(l-imidazolyl) pentyloxyphenoxy-2, 2-dimethylhexanoate hydrochloride (YM534) is a new synthetic anti-tumor compound. Combinations of YM534 with other anti-cancer agents were examined to ascertain whether YM534 potentiated other anti-cancer agents against the KB cell line and its multidrug-resistant counterpart, VJ-300. YM534 potentiated the cytotoxic action of vincristine and actinomycin D about 2-fold against KB cells, but not those of daunomycin and adriamycin. By contrast, YM534 only slightly reversed drug-resistance to adriamycin and daunomycin in VJ-300 while it reversed 5-fold vincristine resistance and 60-fold actinomycin D resistance in VJ-300. The reversal effect of YM534 on actinomycin D and vincristine-resistance in VJ-300 cells appeared to be due to enhanced accumulation of [3H] actinomycin D and [3H] vincristine in VJ-300 cells by YM534. YM534 inhibited efflux of actinomycin D and vincristine from VJ-300 cells, and it also enhanced cellular uptake of these anti-cancer agents. YM534 enhanced cellular accumulation of both actinomycin D and vincristine in the sensitive KB cells. YM534 is thus a unique anti-cancer agent since combinations of other anti-cancer agents with YM534 are expected to augment anti-tumor activity of them. By contrast, YM212, a carboxy analog of YM534, had much less activity to potentiate vincristine and actinomycin D). YM534 at 100-1000 microM almost completely inhibited the photoaffinity labeling of [3H] azidopine to the 170-kD P-glycoprotein of VJ-300 cell membranes, but YM212 showed much less inhibitory action on the photoaffinity labeling. YM534 could also inhibit the photoaffinity labeling of deglycosylated P-glycoprotein.

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Indication	Highest Phase	Country/Location	Organization	Date
Lymphoma	Phase 1	-	Astellas Pharma, Inc.	-

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