Thompson Emily L, Murphy Kevin G
Imperial College London, Faculty of Medicine, Department of Investigative Medicine, Commonwealth Building, Hammersmith Hospital, Du Cane Road, London, W12 0NN, UK.
Curr Opin Investig Drugs. 2010 Apr;11(4):432-9.
The kisspeptin/kisspeptin receptor (KISS1R) system is a critical regulator of reproductive function. The kisspeptins are potent stimulators of the hypothalamic-pituitary-gonadal (HPG) axis via their actions ongonadotropin-releasing hormone. Therefore, kisspeptins represent putative drug targets for the treatment of reproductive diseases. Kisspeptins of 10, 13, 14 and 54 amino acids in length have been identified, all of which contain a C-terminal decapeptide that is essential for biological activity. The longest form, kisspeptin-54, may be the most bioactive in vivo. Moreover, the pattern of kisspeptin administration is important; whereas single or intermittent injections of kisspeptin generally stimulate the HPG axis, continuous administration leads to the desensitization of the HPG axis to the effects of the peptide. Several kisspeptin analogs have been developed, and are discussed in relation to their activity at the KISS1R and to their in vivo HPG axis effects.
kisspeptin/kisspeptin受体（KISS1R）系统是生殖功能的关键调节因子。 kisspeptins通过对促性腺激素释放激素的作用，成为下丘脑-垂体-性腺（HPG）轴的有效刺激物。因此，kisspeptins是治疗生殖疾病的潜在药物靶点。已鉴定出长度为10、13、14和54个氨基酸的kisspeptins，它们都含有对生物活性至关重要的C端十肽。最长的形式，即kisspeptin-54，可能在体内具有最高的生物活性。此外，kisspeptin的给药方式很重要；单次或间歇性注射kisspeptin通常会刺激HPG轴，而持续给药会导致HPG轴对该肽的作用产生脱敏。已经开发了几种kisspeptin类似物，并根据它们在KISS1R上的活性及其对体内HPG轴的影响进行了讨论。
