Stability against enzymatic hydrolysis of endomorphin-1 analogues containing β-proline

被引：47

作者：

Cardillo, G

Gentilucci, L

Tolomelli, A

Calienni, M

Qasem, AR

Spampinato, S

机构：

[1] Univ Bologna, Dipartimento Chim G Ciamician, I-40126 Bologna, Italy

[2] Univ Bologna, Dipartimento Farmacol, I-40126 Bologna, Italy

来源：

ORGANIC & BIOMOLECULAR CHEMISTRY | 2003年 / 1卷 / 09期

关键词：

D O I：

10.1039/b301507f

中图分类号：

O62 [有机化学];

学科分类号：

070303 [有机化学]; 081704 [应用化学];

摘要：

The enantiomer of endomorphin-1 (Tyr-Pro-Trp-PheNH(2)) and the analogues containing (S)- or (R)-beta-proline have been synthesized, and their affinities towards mu-opioid receptors have been measured. As expected, the incubations of the different peptides with some commercially available enzymes showed that the presence Of D-residues gave strong resistance towards digestion. The presence of beta-proline alone is sufficient to confer good resistance against the hydrolysis of the biologically strategic Pro-Trp bond.

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页码：1498 / 1502

页数：5

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