PMID: 7516318Mar 1, 1994Paper

Binding of enkephalin/dextran conjugates to opioid receptors

International Journal of Peptide and Protein Research
Y Sasaki-YagiY Imanishi

Abstract

[ala2]Enkephalin molecules were connected to dextran, and the affinities of the enkephalin/dextran conjugates for opioid receptors were studied. Two kinds of enkephalin derivatives, YaGFLGK-NH2 and YaGFLGS'S'PS'S'PS'KP-OMe (S' represents a Sar residue) were prepared. They retained the high affinity of the enkephalin unit toward opioid receptors. On the other hand, receptor affinity of the enkephalin derivative/dextran conjugates became lower than that of the enkephalin derivatives. Fluorescence from the Tyr residue of the conjugates in a buffer solution was less quenched by succinimide than that of the enkephalin derivatives. Therefore, in these conjugates, the binding of the enkephalin moieties to receptors should be hindered by a steric effect of the dextran matrix. However, the receptor affinity (as defined on the basis of an enkephalin unit) increased on increasing the amount of enkephalin units connected to the dextran matrix, especially in the case of the connection through a shorter spacer arm, suggesting simultaneous binding to a few receptors by the conjugate.

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Citations

Jul 1, 1996·International Journal of Peptide and Protein Research·S TetsuiY Imanishi
Jul 1, 1996·Journal of Peptide Science : an Official Publication of the European Peptide Society·J ZhaoY Imanishi
Jul 25, 1996·Biochimica Et Biophysica Acta·J ZhaoY Imanishi
Sep 1, 2000·Advanced Drug Delivery Reviews·S P Vyas, V Sihorkar
Jan 9, 2001·Trends in Biotechnology·J Gariépy, K Kawamura
Dec 10, 1998·European Journal of Pharmaceutical Sciences : Official Journal of the European Federation for Pharmaceutical Sciences·K YanoY Imanishi

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