Fsh receptor-binding inhibitor fragment(bi-10)

FSH receptor-binding inhibitor fragment(bi-10) is a potent FSH antagonist. FSH receptor-binding inhibitor fragment(bi-10) blocks the binding of FSH to FSHR, and alteres FSH action at the receptor level. FSH receptor-binding inhibitor fragment(bi-10) results in the suppression of ovulation and causes follicular atresia of mice. FSH receptor-binding inhibitor fragment(bi-10) has the potential for utilizing to restrain the carcinogenesis of ovarian cancer by down-regulating overexpression of FSHR and ERβ in the ovaries[1].

Signaling Pathways >> GPCR/G Protein >> GNRH Receptor

Research Areas >> Endocrinology

FSH receptor-binding inhibitor fragment(bi-10) (10, 20, 30, 40 mg/kg; 肌肉注射; 每天1次; 连续5天) 在大剂量 (30 mg/kg-40 mg/kg) 可抑制卵巢和卵泡发育，降低卵巢中 ERβ 和 FSHR mRNA 和蛋白质的表达水平，抑制 E2 的产生[1]。 Animal Model: Prepuberty Kunming female mice of 21-days old and body weight of 22.3±1.52g[1] Dosage: 10, 20, 30, 40 mg/kg Administration: Intramuscularly injection; once a day for five consecutive days Result: Could attenuate FSH promoting effect on the follicular development, resulting in the poor maturation of ovarian follicles. High dose (40mg/kg) treatment blocked the follicle development of mice. High dose of FRBI (40mg/kg) treatment blocked the follicle development of mice.

[1]. Gong Zhuandi, et al. FSH receptor binding inhibitor restrains follicular development and possibly attenuates carcinogenesis of ovarian cancer through down-regulating expression levels of FSHR and ERβ in normal ovarian tissues. Gene. 2018 Aug 20;668:174-181.