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001-es BibID:	BIBFORM033541
035-os BibID:	WOS:000236362600052
Első szerző:	Zarándi Márta
Cím:	Lipopeptide antagonists of growth hormone-releasing hormone with improved antitumor activities / Marta Zarandi, Jozsef L. Varga, Andrew V. Schally, Judit E. Horvath, Gabor L. Toller, Magdolna Kovacs, Markus Letsch, Kate Groot, Patricia Armatis, Gabor Halmos
Dátum:	2006
ISSN:	0027-8424
Megjegyzések:	Antagonists of growth hormone-releasing hormone (GHRH) synthesized previously inhibit proliferation of various human cancers, but derivatisation with fatty acids could enhance their clinical efficacy. We synthesized a series of antagonists of GHRH(1-29)NH2 acylated at the N terminus with monocarboxylic or alpha,omega-dicarboxylic acids containing six to sixteen carbon atoms. These peptides are analogs of prior potent antagonists JV-1-36, JV-1-38, and JV-1-65 with phenylacetyl group at their N terminus. Several new analogs, including MZ-J-7-46 and MZA-7-30, more effectively inhibited GHRH-induced GH release in vitro in a superfused rat pituitary system than their parent compound JV-1-36 and had increased binding affinities to rat pituitary GHRH receptors, but they showed weaker inhibition of GH release in vivo than JV-1-36. All antagonists acylated with fatty acids containing 8-14 carbon atoms inhibited the proliferation of MiaPaCa-2 human pancreatic cancer cells in vitro better than JV-1-36 or JV-1-65. GHRH antagonist MZ-J-7-114 (5 mu g/day) significantly suppressed the growth of PC-3 human androgen-independent prostate cancers xenografted into nude mice and reduced serum lGF-I levels, whereas antagonist JV-1-38 had no effect at the dose of 10 mu g/day. GHRH antagonists including MZ-J-7-46 and MZ-J-7-114 acylated with octanoic acid and MZ-J-7-30 and MZ-J-7-110 acylated with 1,12-dodecanedicarboxylic acid represent relevant improvements over earlier antagonists. These and previous results suggest that this class of GHRH antagonists might be effective in the treatment of various cancers.
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. - 103 : 12 (2006), p. 4610-4615. -
További szerzők:	Varga József L. Schally, Andrew Victor Horváth Judit E. (New Orleans) Toller Gábor L. Kovács Magdolna Letsch, Markus Groot, Kate Armatis, Patricia Halmos Gábor (1962-) (gyógyszerész, receptorfarmakológus, experimentális onkológus)
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