| Title | A new generation of peptide antagonists of substance P | |
| Author | Constantine PoulosDepartment of Chemistry, University of Patras, Patras, Greece | |
| Citation | Poulos, C.: A new generation of peptide antagonists of substance P, Epitheorese Klin. Farmakol. Farmakokinet. 9(2-3): 95-97 (1995) | |
| Publication Date | 1995 | |
| Full Text Language | English | |
| Order – Buy | Ηλεκτρονική Μορφή: pdf (10 €) – Digital Type: pdf (10 €) pharmakonpress[at]pharmakonpress[.]gr | |
| Keywords | Peptide antagonists, substance P. | |
| Other Terms | review article | |
| Summary | The classical approach to substance P (SP) antagonists, in various tachykinin receptors, involves replacement of at least two amino acid residues by D-amino acids at positions 7 and 9 of SP. Modifications at position 11 in the above antagonists improve their affinity although these modifications themselves do not induce antagonism. We have synthesized a new class of SP antagonists, without using D-amino acids, by modifying only the Met11 residue. Thus, replacement of the SCH3 and the α-carboxamide groups of Met11, in the model hexapeptide [Orn6]SP6-11, by benzyl ester groups yielded the analogue [Orn6, Glu(OBz)11]- SP6-11 OBzl which was a potent NK-1 antagonist. Further studies showed that antagonism can be induced in the C-terminal hexapeptide of SP, without using D-amino acids, and the necessary condition was the presence of two phenyl rings at the residue 11, one at the side chain and one at the α-carboxy group. The position of the phenyl ring at the side chain of residue 11 of SP may affect the activity and/or the selectivity of the corresponding antagonist. | |
| References | 1. Regoli, D., Escher, E., Mizrahi J.: Pharmacology : 301-320 (1984)2. Jukic, D., Rouissi, N., Laprlse, R., Boussougou, M., Regoli, D.: Life Sciences 49: 1463-1469 (1991)
3. Karagiannls, K., Manolopoulou, A., Stavropoulos, G., Poulos, C., Jordan, C.C., Hagan, R.M.: Int. J. Pept. Prot. Res. 38: 350-356 (1991) 4. Antoniou, M., Poulos, C., Tsegenidls, T.: Int. J. Pept. Prot. Res. 40: 395-400 (1992) 5. Manolopoulou, A., Poulos, C., Tsegenidis, T.: Eur. J. Med. Chem. 27: 949-954 (1992) 6. Karagiannis, K., Stavropoulos, G., Poulos, C., Jordan, G.C., Hagan, R.M.: Int. J. Pept. Prot. Res. 42: 565-569 (1993) 7. Rouissi, N., Gitter, B.D., Waters, D.C., Howbert, J.J., Nixon, J.A., Regoli, D.: Biochem. Biophys. Res. Comm. 176: 894-901 (1991) 8. Howson, W., Hodgson, J., Richardson, R., Walton, L., Guard, S., Waiting, K.: Bioorgan. Med. Chem. Letters 2(6): 559-564 (1992) |
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Online ISSN 1011-6575
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Articles published in this Journal are Indexed or Abstracted in: • Chemical Abstracts • Elsevier’s Bibliographic Databases: Scopus, EMBASE, EMBiology, Elsevier BIOBASE SCImago Journal and Country Rank Factor
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