Beta-sulfonamido gonadotropin-releasing hormone analogs: synthesis and evaluation of several parent hormone properties. (Articolo in rivista)

Type
Label
  • Beta-sulfonamido gonadotropin-releasing hormone analogs: synthesis and evaluation of several parent hormone properties. (Articolo in rivista) (literal)
Anno
  • 2005-01-01T00:00:00+01:00 (literal)
Http://www.cnr.it/ontology/cnr/pubblicazioni.owl#doi
  • 10.1002/psc.596 (literal)
Alternative label
  • Di-Segni S.; Giordano C.; Rahimipour S.; Ben-Aroya N.; Koch Y.; Fridkin M. (2005)
    Beta-sulfonamido gonadotropin-releasing hormone analogs: synthesis and evaluation of several parent hormone properties.
    in Journal of peptide science (Print)
    (literal)
Http://www.cnr.it/ontology/cnr/pubblicazioni.owl#autori
  • Di-Segni S.; Giordano C.; Rahimipour S.; Ben-Aroya N.; Koch Y.; Fridkin M. (literal)
Pagina inizio
  • 45 (literal)
Pagina fine
  • 52 (literal)
Http://www.cnr.it/ontology/cnr/pubblicazioni.owl#numeroVolume
  • 11 (literal)
Rivista
Http://www.cnr.it/ontology/cnr/pubblicazioni.owl#numeroFascicolo
  • 1 (literal)
Note
  • Scopu (literal)
  • ISI Web of Science (WOS) (literal)
Http://www.cnr.it/ontology/cnr/pubblicazioni.owl#affiliazioni
  • Departments of Organic Chemistry and Neurobiology, The Weizmann Institute of Science, Rehovot, Israel 76100 Istituto di Chimica Biomolecolare del CNR, Sezione di Roma c/o, Dipartimento di Studi Farmaceutici, Universita degli Studi di Roma 'La Sapienza', Roma, Italy. (literal)
Titolo
  • Beta-sulfonamido gonadotropin-releasing hormone analogs: synthesis and evaluation of several parent hormone properties. (literal)
Abstract
  • With the aim of producing long-acting analogs of gonadotropin releasing hormone (GnRH), four analogs, containing -X6aa?(CH2SO2NH)-Leu7 building unit (Xaa Gly, Ala, Val or Phe), and a reduced-size analog[Des-Tyr5]-GnRH which includes the unit Phe5?(CH2SO2NH)-Leu6, and [?-Ala6]-GnRH were synthesized. The peptides were evaluated for their capacity to induce LH-release from rat pituitary cells and to withstand proteolysis by pituitary-derived enzymes, compared with the parent peptide GnRH. Albeit stable toward enzymatic degradation, the sulfonamido containing peptides were only marginally bioactive. [?-Ala6]-GnRH, however, induced LH-release and bound to pituitary receptors nearly as efficiently as GnRH. This analog was also highly stable toward proteolysis suggesting that it may serve as a long-acting GnRH-analog. (literal)
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