生物活性 | |||
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描述 | Gonadotropin-releasing-hormone (GnRH) analogues are synthetic compounds derived from decapeptide neurohormones (LHRH; LH/FSH-RH). They have a key role in hormone dependent cancer, particularly breast and prostate cancer(i.e. ovariectomy and orchiectomy), providing an androgen and estrogen ablation. GnRH exert an inhibitory action on the growth of hormone-dependent human and canine mammary tumor[3]. The GnRH receptor rather interacts with the mitogenic signal transduction of growth-factor receptors and related oncogene products associated with tyrosine kinase activity via activation of a phosphotyrosine phosphatase resulting in downregulation of cancer cell proliferation[4]. GnRH analogues counteract the proliferating effects of both epidermal growth factor (EGF) and insulin like growth factor (IGF-I); additionally, it affects the mitogen-activated protein kinase (MAPK) cascade and modulates the activity of the urokinase-type plasminogen activator (uPA)/plasminogen activator inhibitory (PAI) system, which is involved in the process of metastasis[5]. Fertirelin, an analog of GnRH 2.5 to 10 times more potent than native GnRH, has become the treatment of choice for reversing follicular cysts[6]. Administration of high doses of Fertirelin is found to reduce superovulatory responses[7]. |
实验方案 | |||
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1mg | 5mg | 10mg | |
1 mM 5 mM 10 mM |
0.87mL 0.17mL 0.09mL |
4.34mL 0.87mL 0.43mL |
8.67mL 1.73mL 0.87mL |
参考文献 |
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[3]Salvatore Florio,et al. GnRH and steroids in cancer. Front Biosci. 2002 Jun 1;7:d1590-608. |