This paper reports data on the design, the conformational features and the pharmacological properties of the bicyclic peptide tachykinin NK2 receptor antagonist MEN 10,627 or cyclo(Met-Asp-Trp-Phe-Dap-Leu)cyclo(2 beta-5 beta). MEN 10,627 possesses a highly constrained structure characterized by two consecutive beta-turns, as confirmed by the almost coincident results of NMR and X-ray analyses. The compound has been efficiently synthesized by solid-phase methodology using either Boc or Fmoc strategies. It is quite stable to metabolic degradation and is endowed with high affinity and selectivity for NK2 receptor expressed in various species.
A Review of the Design, Synthesis and Biological Activity of the Bicyclic Hexapeptide Tachykinin NK2 antagonist MEN 10627 / L., Quartara; Pavone, Vincenzo; C., Pedone; Lombardi, Angelina; A. R., Renzetti; C. A., Maggi. - In: REGULATORY PEPTIDES. - ISSN 0167-0115. - STAMPA. - 65:(1996), pp. 55-59. [10.1016/0167-0115(96)00072-9]
A Review of the Design, Synthesis and Biological Activity of the Bicyclic Hexapeptide Tachykinin NK2 antagonist MEN 10627
PAVONE, VINCENZO;LOMBARDI, ANGELINA;
1996
Abstract
This paper reports data on the design, the conformational features and the pharmacological properties of the bicyclic peptide tachykinin NK2 receptor antagonist MEN 10,627 or cyclo(Met-Asp-Trp-Phe-Dap-Leu)cyclo(2 beta-5 beta). MEN 10,627 possesses a highly constrained structure characterized by two consecutive beta-turns, as confirmed by the almost coincident results of NMR and X-ray analyses. The compound has been efficiently synthesized by solid-phase methodology using either Boc or Fmoc strategies. It is quite stable to metabolic degradation and is endowed with high affinity and selectivity for NK2 receptor expressed in various species.I documenti in IRIS sono protetti da copyright e tutti i diritti sono riservati, salvo diversa indicazione.
