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Luliberyna, jej analogi oraz lutropina

Szewczuk A., Kurowska E.

Wiadomości Chemiczne

1999

[Z] 53, 3-4

219-234

The mammalian hormone (or factor) which releases luteinizing hormone (LH, lutropin) and follicle stimulating hormone (FSH, follitropin) was isolated from ovine and porcine hypothalami and identified as decapeptide with the following sequence: pGlu1-His2-Trp3-Ser4-Tyr5-Gly6-Leu7-Arg8-Pro9-Gly10-NH2. For synthesis of the luliberin (luteinizing hormone releasing hormone, LH-RH) and its analogs solid phase Merriefield technique and for puriffication reverse phase HPLC were usually applied. Until now thousands of LH-RH analogs were synthesized and some of them were applied in gynecology and oncology. Such achievements were possible through replacing proteinic L-amino acids in LH-RH molecule for nonproteinic synthetic, D-amino acids. The luliberin called also gonadoliberin (Gn-RH) plays an important role as regulator of reproduction. Secretion of lutropin (LH) by anterior pituitary celles in an pulsative manner is controlled by pulsative relese of LH-RH from hypothalamus. It was well established that the surge of LH at midcycle in woman urines is an authentic predicator of approaching ovulation. In gonades LH stimulates synthesis of sex steroid hormones. The well known luliberin analogs were: Buserelin (Suprefact), Zoladex (Goserelin) and Cetrorelix (SB75). They were applied for treatment of prostatic, ovarian and breast cancers, endometriosis and in vitro fertilization.