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首页> 外文期刊>Proceedings of the National Academy of Sciences of the United States of America >Recovery of pituitary function after treatment with a targeted cytotoxic analog of luteinizing hormone-releasing hormone
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Recovery of pituitary function after treatment with a targeted cytotoxic analog of luteinizing hormone-releasing hormone

机译:黄体生成素释放激素的靶向细胞毒性类似物治疗后垂体功能的恢复

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摘要

Recently, we developed a targeted cytotoxic analog AN-207 of luteinizing hormone-releasing hormone (LH-RH), consisting of an intensely potent derivative of doxorubicin, 2-pyrrolinodoxorubicin (AN-201) conjugated to carrier agonist [D-Lys]LH-RH. In this study, we investigated the effects of cytotoxic analog AN-207, designed for targeted chemotherapy and radical AN-201 on pituitary function in rats. A selective damage to the pituitary gonadotroph cells was found at 1 week after a single i.v. injection of 150 nmol/kg AN-207, as evidenced by a 63/100 decrease in the LH-RH- stimulated release of LH in vitro.
机译:最近,我们开发了一种促黄体生成激素释放激素(LH-RH)的靶向细胞毒类似物AN-207,其由与载体激动剂[D-Lys] LH缀合的阿霉素,2-吡咯啉/阿霉素(AN-201)的强效衍生物组成-RH。在这项研究中,我们调查了细胞毒性类似物AN-207(为靶向化疗而设计)和自由基AN-201对大鼠垂体功能的影响。一次静脉注射后1周发现对垂体促性腺激素细胞的选择性损伤。注射150 nmol / kg AN-207,如LH-RH刺激的体外LH释放降低63/100所证明。

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