Spasmogenic activity of chemotactic N-formylated oligopeptides: identity of structure--function relationships for chemotactic and spasmogenic activities.
Spasmogenic activity of chemotactic N-formylated oligopeptides: identity of structure--function relationships for chemotactic and spasmogenic activities.
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趋化N-甲酰化寡肽的痉挛活性：趋化和痉挛活性的结构-功能关系的同一性。
DOI：
10.1073/pnas.79.23.7470
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发表时间：
1982
影响因子：
11.1
通讯作者：
Ward,PA
中科院分区：
文献类型：
--
作者：
Marasco,WA;Fantone,JC;Ward,PA
趋化性N-甲酰基化寡肽是豚鼠回肠的强效痉挛剂。各种N-甲酰化肽的结构-活性研究表明存在一种特异性受体，其特异性类似于白细胞上的甲酰肽受体。白细胞上甲酰基肽受体的竞争性拮抗剂也抑制甲酰基肽诱导的回肠收缩，而抗组胺剂苯海拉明则没有作用。由合成的N-甲酰化肽引起的收缩反应不同于由乙酰胆碱、组胺和P物质诱导的收缩反应。特别地，在反应开始之前观察到用N-甲酰化肽处理后的潜伏期，并且不维持持续的收缩反应。此外，快速耐受确实发生，但在20- 30分钟的休息期后可以看到活动的完全恢复。这些观察结果表明，广泛的生物学作用的原核信号肽从细菌作为急性炎症介质。
The chemotactic N-formylated oligopeptides are potent spasmogenic agents for guinea pig ileum. Structure-activity studies with various N-formylated peptides suggest the presence of a specific receptor that resembles in specificity the formyl peptide receptor on leukocytes. A competitive antagonist of the formyl peptide receptor on leukocytes also inhibits formyl peptide-induced ileum contraction, whereas the antihistamine diphenhydramine is without effect. The contractile response caused by the synthetic N-formylated peptides differs from those induced by acetylcholine, histamine, and substance P. In particular, a latent period after treatment with the N-formyl peptides is seen before the onset of the response, and a sustained contractile response is not maintained. In addition, tachyphylaxis does occur, but complete recovery of activity is seen after a 20- to 30-min rest period. These observations suggest broad biological roles of prokaryotic signal peptides from bacteria as acute inflammatory mediators.