In vivo andin vitro antitumor activity of mitomycin C conjugates at 7-N position through a linker containing thiocarbamate bond with CD10 monoclonal antibody
In vivo andin vitro antitumor activity of mitomycin C conjugates at 7-N position through a linker containing thiocarbamate bond with CD10 monoclonal antibody
复制标题
含硫代氨基甲酸酯键的丝裂霉素 C 7-N位缀合物与 CD10 单克隆抗体的体内和体外抗肿瘤活性
DOI:
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发表时间:
1992
期刊:
影响因子:
--
通讯作者:
Toshitada Takahashi
中科院分区:
文献类型:
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作者:
Y. Shida;M. Okabe;T. Kuroda;Makoto Morimotol;R. Ueda;Toshitada Takahashi
AbstractThrough a linker containing thiocarbomate bound to the 7-N position of mitomycin C (MMC), conjugates with a monoclonal antibody to CD10 (NL-1) were prepared, and their antitumor activities were examined. All five conjugates, except one, showedin vitro cytotoxity to two CD10+ lymphoid cell lines superior to MMC. The conjugate displaying the highest cytotoxicity was selected and further tested against three CD10+ and two CD10 lymphoid cell linesin vitro. The conjugate with NL-1 antibody demonstrated higher cytotoxic activity against CD10+ tumor cells than the control conjugate with normal immunoglobulin, while there was no significant difference, when tested against CD10− tumors. The cytotoxic activity of the NL-1 conjugate to CD10+ tumors was significantly blocked by NL-1 antibody.
In vivo antitumor activity of the NL-1 conjugate was then tested against a CD10+ tumor transplanted to nude mice, and side effects were recorded. The NL-1 conjugate (4 mg/kg) showed anin vivo antitumor effect similar to MMC (2 mg/kg), which is at nearly maximal tolerable dose; the latter induced decreases in numbers of leukocytes and platelets, while the former did not, suggesting less side effect by the NL-1 conjugate. Since MMC demonstrates a broad spectrum of antitumor activity, the conjugate, as such, may be applicable for the treatment of cancer patients.
影响因子:
56.9
作者:
E. Vitetta;R. Fulton;R. May;M. Till;J. Uhr
通讯作者:
E. Vitetta;R. Fulton;R. May;M. Till;J. Uhr
影响因子:
7.3
作者:
Iyengar,BS;Sami,SM;Remers,WA;Bradner,WT;Schurig,JE
通讯作者:
Schurig,JE
影响因子:
7.3
作者:
Sami,SM;Iyengar,BS;Tarnow,SE;Remers,WA;Bradner,WT;Schurig,JE
通讯作者:
Schurig,JE