Cavicchioni Giorgio, Fraulini Anna, Falzarano Sofia, Spisani Susanna
Department of Pharmaceutical Sciences, University of Ferrara, 44100 Ferrara, Italy.
Bioorg Chem. 2006 Oct;34(5):298-318. doi: 10.1016/j.bioorg.2006.07.001. Epub 2006 Aug 17.
Neutrophils constitute the first line of defence against bacterial invasion. They migrate to infected tissues along a concentration gradient of chemoattractant molecules, the most important of which is for-Met-Leu-Phe-OH (fMLP). Different responses arise from formylpeptides binding to different isoforms of the specific receptor. The aim of the studies reported herein was to clarify (i) the role of fMLP-OMe amide bonds in receptor-ligand cross-linking, (ii) the nature of the group occupying the N- and C-terminal positions, (iii) the features peculiar to the Met, Leu, and Phe receptor pockets, and (iv) the features which determine the specific neutrophil response.
中性粒细胞构成了抵御细菌入侵的第一道防线。它们沿着趋化因子分子的浓度梯度迁移到感染组织，其中最重要的趋化因子是甲酰甲硫氨酰-亮氨酰-苯丙氨酸-OH（fMLP）。甲酰肽与特定受体的不同亚型结合会产生不同的反应。本文报道的研究目的是阐明：（i）fMLP-OMe酰胺键在受体-配体交联中的作用；（ii）占据N端和C端位置的基团的性质；（iii）甲硫氨酸、亮氨酸和苯丙氨酸受体口袋的独特特征；以及（iv）决定中性粒细胞特异性反应的特征。
