Blossey H C, Gayer B, Amir-Zaltsman Y, Kohen F
Mol Cell Endocrinol. 1986 Aug;46(3):245-52. doi: 10.1016/0303-7207(86)90006-7.
Conjugates of ovine prolactin and daunomycin were prepared for use as affinity-labelled drug carriers in cancer cells carrying the prolactin receptor. The binding affinity of the conjugates to prolactin receptors in rat liver membrane preparations and in viable granulosa cells derived from estradiol- and pregnant mare serum gonadotropin (PMSG)-treated immature female rats was less than an order of magnitude lower than prolactin. The toxicity of the conjugate in cultured granulosa cells was dependent upon the concentration of the daunomycin present in the culture. The cytotoxic effect of the ligand was abolished by the addition of free prolactin or NH4Cl to the granulosa cell cultures. These conjugates may be useful probes in drug targeting against hormone-sensitive cancer.
制备了绵羊催乳素与柔红霉素的偶联物，用作携带催乳素受体的癌细胞中的亲和标记药物载体。这些偶联物对大鼠肝膜制剂以及来自经雌二醇和孕马血清促性腺激素（PMSG）处理的未成熟雌性大鼠的活颗粒细胞中催乳素受体的结合亲和力，比催乳素低不到一个数量级。偶联物在培养的颗粒细胞中的毒性取决于培养物中柔红霉素的浓度。向颗粒细胞培养物中添加游离催乳素或氯化铵可消除配体的细胞毒性作用。这些偶联物可能是针对激素敏感性癌症进行药物靶向治疗的有用探针。
