Synthesis and evaluation of RGD peptidomimetics aimed at surface bioderivatization of polymer substrates
Synthesis and evaluation of RGD peptidomimetics aimed at surface bioderivatization of polymer substrates
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DOI：
10.1016/s0968-0896(98)00083-2
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发表时间：
1998-09-01
影响因子：
3.5
通讯作者：
Marchand-Brynaert, J
中科院分区：
文献类型：
--
作者：
Boxus, T;Touillaux, R;Marchand-Brynaert, J
已经以收敛的方式从常见的邻氨基酪氨酸模板（用锚定臂或甲基O-取代，和用氟标签α N-取代用于XPS分析）和各种ω-氨基酸衍生物制备了几种RGD肽模拟物。在血小板聚集试验中，最灵活的化合物显示出与肽参比品（RGDS）相似的生物活性。化合物16 a可以与作为整合素的良好配体的两种环肽----β 728和c（RGDfV）拟合（通过模型化）。化合物16 b已共价固定在用作哺乳动物细胞培养支持物的聚（对苯二甲酸乙二醇酯）膜的表面上。(C)1998爱思唯尔科技有限公司版权所有。
Several RGD peptidomimetics have been prepared, in a convergent way, from the common ortho-amino-tyrosine template (O-substituted with an anchorage-arm or a methyl group, and alpha N-substituted with a fluorine tag for XPS analysis), and various omega-aminoacid derivatives. The most flexible compounds have shown a biological activity similar to that of the peptide reference (RGDS) in the platelet aggregation test. The compound 16a could be fitted (by modelisation) with DMP 728 and c(RGDfV), two cyclic peptides that are good ligands of integrins. The compound 16b has been covalently fixed on the surface of a poly(ethylene terephthalate) membrane used as support for mammalian cell cultivation. (C) 1998 Elsevier Science Ltd. All rights reserved.