Pagani Zecchini G, Torrini I, Paglialunga Paradisi M, Lucente G, Spisani S
Dipartimento di Studi Farmaceutici, Università La Sapienza, Roma.
Farmaco. 1994 Nov;40(11):739-42.
For-Met-delta ZLeu-delta ZPhe-OMe (3) has been synthesized as a new analogue of the prototypical chemotactic agent For-Met-Leu-Phe-OMe (fMLP-OMe). Compound 3 is characterized by presence of two consecutive alpha,beta-didehydro amino acid residues [delta ZLeu = (Z)-alpha,beta-didehydroleucine; delta ZPhe = (Z)-alpha,beta- didehydrophenylalanine] located at the central and C-terminal position, respectively. When tested on human neutrophils the N-formyltripeptide 3, although less active than the parent, is able to induce chemotaxis, superoxide anion production and lysozyme release. The activity of 3 has been compared to that of related fMLP-OMe analogues containing a single delta ZPhe residue located at the C-terminal position.
已合成了For-Met-delta ZLeu-delta ZPhe-OMe（3）作为原型趋化剂For-Met-Leu-Phe-OMe（fMLP-OMe）的一种新类似物。化合物3的特征在于分别位于中央和C末端位置的两个连续的α，β-脱氢氨基酸残基[delta ZLeu =（Z）-α，β-脱氢亮氨酸；delta ZPhe =（Z）-α，β-脱氢苯丙氨酸]的存在。当在人中性粒细胞上进行测试时，N-甲酰三肽3虽然活性低于母体，但能够诱导趋化性、超氧阴离子产生和溶菌酶释放。已将3的活性与含有位于C末端位置的单个delta ZPhe残基的相关fMLP-OMe类似物的活性进行了比较。
