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Titolo:
Antagonistic actions of analogs related to growth hormone-releasing hormone (GHRH) on receptors for GHRH and vasoactive intestinal peptide on rat pituitary and pineal cells in vitro
Autore:
Rekasi, Z; Varga, JL; Schally, AV; Halmos, G; Groot, K; Czompoly, T;
Indirizzi:
Tulane Univ, Sch Med, Inst Endocrine Polypeptide & Canc, Vet Affairs Med Ctr, New Orleans, LA 70112 USA Tulane Univ New Orleans LA USA 70112 s Med Ctr, New Orleans, LA 70112 USA Tulane Univ, Sch Med, Dept Med, New Orleans, LA 70112 USA Tulane Univ NewOrleans LA USA 70112 Dept Med, New Orleans, LA 70112 USA
Titolo Testata:
PROCEEDINGS OF THE NATIONAL ACADEMY OF SCIENCES OF THE UNITED STATES OF AMERICA
fascicolo: 3, volume: 97, anno: 2000,
pagine: 1218 - 1223
SICI:
0027-8424(20000201)97:3<1218:AAOART>2.0.ZU;2-3
Fonte:
ISI
Lingua:
ENG
Soggetto:
CYCLASE-ACTIVATING POLYPEPTIDE; ADENYLATE-CYCLASE; FACTOR GRF; STRUCTURAL REQUIREMENTS; MELATONIN SECRETION; SUPERFUSION SYSTEM; POTENT ANTAGONISTS; MOLECULAR-CLONING; VIP RECEPTORS; INVITRO;
Keywords:
growth hormone-releasing hormone and vasoactive intestinal peptide antagonists; structure-activity relationships; cancer therapy;
Tipo documento:
Article
Natura:
Periodico
Settore Disciplinare:
Life Sciences
Citazioni:
37
Recensione:
Indirizzi per estratti:
Indirizzo: Schally, AV Tulane Univ, Sch Med, Inst Endocrine Polypeptide & Canc, Vet Affairs Med Ctr, 1430 Tulane Ave, New Orleans, LA 70112 USA Tulane Univ 1430Tulane Ave New Orleans LA USA 70112 70112 USA
Citazione:
Z. Rekasi et al., "Antagonistic actions of analogs related to growth hormone-releasing hormone (GHRH) on receptors for GHRH and vasoactive intestinal peptide on rat pituitary and pineal cells in vitro", P NAS US, 97(3), 2000, pp. 1218-1223

Abstract

Peptide analogs of growth hormone-releasing hormone (GHRH) can potentiallyinteract with vasoactive intestinal peptide (VIP) receptors (VPAC(1)-R andVPAC(2)-R) because of the structural similarities of these two hormones and their receptors. We synthesized four new analogs related to GHRH (JV-1-50, JV-1-51, JV-1-52, and JV-1-53) with decreased GHRH antagonistic activity and increased VIP antagonistic potency. To characterize various peptide analogs for their antagonistic activity on receptors for GHRH and VIP, we developed assay systems based on superfusion of rat pituitary and pineal cells. Receptor-binding affinities of peptides to the membranes of these cells were also evaluated by radioligand competition assays. Previously reported GHRH antagonists JV-1-36, JV-1-38, and JV-1-42 proved to be selective for GHRH receptors, because they did not influence VIP-stimulated VPAC(2) receptor-dependent prolactin release from pituitary cells or VPAC(1) receptor-dependent cAMP efflux from pinealocytes but strongly inhibited GHRH-stimulated growth hormone (GH) release. Analogs JV-1-50, JV-1-51, and JV-1-52 showed various degrees of VPAC(1)-R and VPAC(2)-R antagonistic potency, although also preserving a substantial GHRH antagonistic effect. Analog JV-1-53 proved to be a highly potent VPAC(1) and VPAC(2) receptor antagonist, devoid of inhibitory effects on GHRH-evoked GH release. The antagonistic activity of these peptide analogs on processes mediated by receptors for GHRH and VIP wasconsistent with the binding affinity. The analogs with antagonistic effects on different types of receptors expressed on tumor cells could be utilized for the development of new approaches to treatment of various human cancers.

ASDD Area Sistemi Dipartimentali e Documentali, Università di Bologna, Catalogo delle riviste ed altri periodici
Documento generato il 15/07/20 alle ore 14:50:51