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Conformation-activity relationship in hexapeptides related to substance P
J Elguero1, J M García-Antón, P Goya
1Instituto de Quimica Médica Consejo Superior de Investigaciones Cientificas, Madrid, Spain.
Arzneimittel-Forschung
|August 1, 1989
Abstract:
Two hexapeptides related to the undecapeptide substance P (SP) Glu-Phe-Phe-Gly-Leu-Met-NH2 and Glu-Phe-Phe-Pro-Leu-Met-NH2, have been synthesized and their selectivity for the SP receptors studied. Conformational analyses of both peptides have been carried out using a molecular modeling program. Activity appears to be related to the adoption of a U-shape conformation since the Pro9 containing peptide in which this folding is favoured is much more active than the hexapeptide containing Gly9. Moreover, such a substitution induces a significant selectivity for the SP-P receptor compared to the SP-E receptor.