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001-es BibID:	BIBFORM033631
035-os BibID:	(Scopus)0034242518 (WoS)000088208700022 (PMID)10891548
Első szerző:	Halmos Gábor (gyógyszerész, receptorfarmakológus, experimentális onkológus)
Cím:	Down-regulation and change in subcellular distribution of receptors for luteinizing hormone-releasing hormone in OV-1063 human epithelial ovarian cancers during therapy with LH-RH antagonist Cetrorelix / Gábor Halmos, Andrew V. Schally, Zsuzsanna Kahan
Dátum:	2000
Megjegyzések:	The inhibition of growth of various hormone-dependent cancers by analogs of luteinizing hormone-releasing hormone (LH-RH) may be exerted in port through receptors for LH-RN present on tumor cells, but the direct mode of action of LH-RH agonists and antagonists is still not completely understood. The aim of this study was to investigate the effects of agonist [D-Trp(6)]LH-RH and antagonist Cetrorelix, administered s.c, at a dose of 100 mu g/day for 3 weeks on the binding characteristics and subcellular localization of receptors for LH-RH in OV-1063 human epithelial ovarian cancers xenografted into nude mice. Using radioligand binding studies, following in vitro desaturation, we demonstrated the presence of specific, high affinity binding sites for LH-RH in both cell membrane and nuclear fraction of OV-1063 tumors. Treatment with Cetrorelix, but not [D-Trp(6)]LH-RH, caused about 60% reduction (p<0.01) in tumor volume and weight. [D-Trp(6)]LH-RH decreased the number of LH-RN receptors on OV-1063 tumor membranes by 44% after 14 days (p<0.01), and the concentration of receptors remained at that level on day 21. The maximal binding capacity of receptors for LH-RH in the nuclei was significantly higher (p<0.05) after 3 weeks of treatment with [D-Trp(6)]LH-RH, Cetrorelix decreased the concentration of membrane receptors for LH-RH by 53% (p<0.01) after 14 days and the levels on day 21 were even lower, showing a 70% reduction (p<0.01). In contrast, the number of LH-RN binding sites in the nuclear pellet was significantly increased (p<0.01) by Cetrorelix at that time. Our results demonstrate for the first time that the down-regulation of LH-RN receptors on the cell membranes of OV-1063 human ovarian cancers after therapy with antagonist Cetrorelix or agonist [D-Trp(6)]LH-RH is associated with an increase in receptor concentration in the nuclei. These phenomena could be related to the internalization and subcellular translocation of receptors in these tumor cells.
Tárgyszavak:	Orvostudományok Gyógyszerészeti tudományok idegen nyelvű folyóiratközlemény külföldi lapban külföldön készült közlemény
Megjelenés:	International Journal of Oncology. - 17 : 2 (2000), p. 367-373. -
További szerzők:	Schally, Andrew Victor Kahán Zsuzsa
Internet cím:	Intézményi repozitóriumban (DEA) tárolt változat
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