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001-es BibID:	BIBFORM033743
035-os BibID:	(Scopus)0026491007 (WoS)A1992JW79800047
Első szerző:	Janáky Tamás
Cím:	Short-chain analogs of luteinizing hormone-releasing hormone containing cytotoxic moieties / T. Janáky, A. Juhász, Z. Rékasi, P. Serfözö, J. Pinski, L. Bokser, G. Srkalovic, S. Milovanovic, T. W. Redding, G. Halmos, A. Nagy, A. V. Schally
Dátum:	1992
ISSN:	0027-8424
Megjegyzések:	Five hexapeptide and heptapeptide analogs of luteinizing hormone-releasing hormone (LH-RH) were synthesized for use as carriers for cytotoxic compounds. These short analogs were expected to enhance target selectivity of the antineoplastic agents linked to them. Native LH-RH-(3-9) and LH-RH-(4-9) containing D-lysine and D-ornithine at position 6 were amidated with ethylamine and acylated on the N terminus. The receptor-binding affinity of one hexapeptide carrier AJ-41 (Ac-Ser-Tyr-D-Lys-Leu-Arg-Pro-NH-Et) to human breast cancer cell membranes was similar to that of [D-Trp6]LH-RH. Alkylating nitrogen mustards (melphalan, Ac-melphalan), anthraquinone derivatives including anticancer antibiotic doxorubicin, antimetabolite (methotrexate), and cisplatin-like platinum complex were linked to these peptides through their omega-amino group at position 6. The hybrid molecules showed no LH-RH agonistic activity in vitro and in vivo but had nontypical antagonistic effects on pituitary cells in vitro at the doses tested. These analogs showed a wide range of receptor-binding affinities to rat pituitaries and cell membranes of human breast cancer and rat Dunning prostate cancer. Several of these conjugates exerted some cytotoxic effects on MCF-7 breast cancer cell line.
Tárgyszavak:	Orvostudományok Gyógyszerészeti tudományok idegen nyelvű folyóiratközlemény külföldi lapban külföldön készült közlemény
Megjelenés:	Proceedings of The National Academy of Sciences of The United States of America. - 89 : 21 (1992), p. 10203-10207. -
További szerzők:	Juhász A. Rékási Zoltán Serfőző P. Pinski, Jacek Bokser, L. Srkalovic, G. Milovanovic, Slobodan Redding, T. W. Halmos Gábor (1962-) (gyógyszerész, receptorfarmakológus, experimentális onkológus) Nagy Attila Schally, Andrew Victor
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