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001-es BibID:	BIBFORM033898
035-os BibID:	(PMID)8008640
Első szerző:	Szőke Balázs
Cím:	LH-RH analogue carrying a cytotoxic radical is internalized by rat pituitary cells in vitro / Balázs Szőke, Judit Horváth, Gábor Halmos, Zoltán Rékási, Kate Groot, Attila Nagy, Andrew V. Schally
Dátum:	1994
ISSN:	0196-9781
Megjegyzések:	The binding and internalization of a cytotoxic analogue of luteinizing hormone-releasing hormone (LH-RH), T-98 (agonist [D-Lys6]LH-RH linked to glutaryl-2-(hydroxymethyl)anthraquinone), by rat anterior pituitary cells was investigated. Analogue T-98 was bound to pituitary membrane binding sites for LH-RH with a high affinity (Kd = 1.2 nM) and was 17 times more potent in releasing luteinizing hormone (LH) from superfused rat pituitary cells than LH-RH. The labeling of this cytotoxic LH-RH analogue was carried out both with radioactive (125I) and nonradioactive iodine. Monoiodination of the Tyr5 residue of T-98 did not significantly affect its binding affinity but greatly decreased its LH-releasing activity to about 3% of the original value. Di-iodination in the same position lowered binding affinity twenty-threefold and further diminished LH-releasing potency. [125I]T-98 was found to bind very strongly to polystyrene, which precluded the use of regular tissue culture plasticware in our experiments. In pituitary cells cultured in glass vials, binding and internalization of [125I]T-98 were observed, which were time and temperature dependent, and which could be inhibited by excess unlabeled analogue. No enzymatic degradation of labeled T-98 was detected in the culture medium during the incubation. Our results indicate that T-98 is internalized by pituitary gonadotropes through receptor-mediated endocytosis. Because this new class of compounds was designed as anticancer drugs, our findings also suggest that this cytotoxic LH-RH agonist may also be internalized by LH-RH receptors present in breast, prostate, ovarian, and other tumors.
Tárgyszavak:	Orvostudományok Gyógyszerészeti tudományok idegen nyelvű folyóiratközlemény külföldi lapban folyóiratcikk külföldön készült közlemény
Megjelenés:	Peptides. - 15 : 2 (1994), p. 359-366. -
További szerzők:	Horváth Judit E. (New Orleans) Halmos Gábor (1962-) (gyógyszerész, receptorfarmakológus, experimentális onkológus) Rékási Zoltán Groot, Kate Nagy Attila Schally, Andrew Victor
Internet cím:	Szerző által megadott URL DOI Intézményi repozitóriumban (DEA) tárolt változat
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