An evaluation of fMLP pocket dimensions and features using formyltetrapeptides

被引：6

作者：

Cavicchioni, G

Varani, K

Niccoli, S

Rizzuti, O

Spisani, S

机构：

[1] Univ Ferrara, Dept Pharmaceut Sci, I-44100 Ferrara, Italy

[2] Univ Ferrara, Pharmacol Sect, Dept Expt & Clin Med, I-44100 Ferrara, Italy

[3] Univ Ferrara, Dept Biochem & Mol Biol, I-44100 Ferrara, Italy

来源：

JOURNAL OF PEPTIDE RESEARCH | 1999年 / 54卷 / 04期

关键词：

binding affinity; formylpeptides; human neutrophils; structure-activity relationship;

D O I：

10.1034/j.1399-3011.1999.00106.x

中图分类号：

Q5 [生物化学];

学科分类号：

071010 ; 081704 ;

摘要：

The formyltetrapeptides for-Met-Leu-Leu-Phe-OMe 1, for-Met-Leu-Aib-Phe-OMe 2, for-Met-Leu-Ac(6)c-Phe-OMe 3, for-Met-Leu-Pro-Phe-OMe 4, for-Met-Pro-Pro-Phe-OMe 5, for-Met-Aib-Aib-Phe-OMe 6, for-Met-Pro-Aib-Phe-OMe 7 and for-Met-Aib-Pro-Phe-OMe 8 were synthesized and biologically tested on human neutrophils in an attempt to evaluate the specific receptor pocket dimensions and features. Our results indicate that the shift in the Phe residue to the fourth position in these compounds strongly reduces chemotactic response, but is efficacious in triggering superoxide anion production and lysozyme release (order of potency 3 > 2 > 1 > 4 > 6 > 8 > 5 > 7). The potency of the two latter responses correlates well with the affinity data obtained in binding experiments.

引用

收藏

页码：336 / 343

页数：8

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