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001-es BibID:	BIBFORM033695
035-os BibID:	PMID:9145431 WOS:A1997WX50100015
Első szerző:	Zarándi Márta
Cím:	Synthesis and in vitro evaluation of new potent antagonists of growth hormone-releasing hormone (GH-RH) / Marta Zarandi, Magdolna Kovacs, Judit E. Horvath, Katalin Toth, Gabor Halmos, Kate Groot, Attila Nagy, Zoltan Kele, Andrew V. Schally
Dátum:	1997
ISSN:	0196-9781
Megjegyzések:	In the search for more potent antagonists of hGH-RH, 20 new analogs were synthesized, purified and tested in vitro. All the analogs were based on the N-terminal sequence of 28 or 29 amino acid residues of hGH-RH, but contained D-Arg2 and Nle27 modifications. Most analogs had Phe (pCl)6 and Agm29 substituents. The effect of other substitutions such as Abu8 and/or Abu15 and Ala15 and various hydrophobic and hydrophilic D or L amino acids at position 8 were also investigated. All the peptides were acylated at the N-terminus in an attempt to increase the antagonistic activity. In the superfused rat pituitary cell system, most analogs inhibited more powerfully the GH release induced by GH-RH than the standard antagonist [Ac-Tyr1, D-Arg2]hGH-RH (1-29)-NH2. Some antagonists were long acting. Among the peptides synthesized, antagonist PhAc[D-Arg2, Phe(pCl)6, Abu15, Nle27]hGH-RH (1-28) Agm (MZ-5-156) appeared to be the most potent and inhibited GH release in vitro 63-200 times more powerfully than the standard antagonist. MZ-5-156 and other antagonists showed high binding affinities to membrane receptors for GH-RH. Some of these hGH-RH antagonists could be further developed for possible onocological applications.
Tárgyszavak:	Orvostudományok Gyógyszerészeti tudományok idegen nyelvű folyóiratközlemény külföldi lapban külföldön készült közlemény
Megjelenés:	Peptides. - 18 : 3 (1997), p. 423-430. -
További szerzők:	Kovács Magdolna Horváth Judit E. (New Orleans) Tóth Katalin Halmos Gábor (1962-) (gyógyszerész, receptorfarmakológus, experimentális onkológus) Groot, Kate Nagy Attila Kele Zoltán Schally, Andrew Victor
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