The synthesis and properties of Gla- and Phe-containing analogues of cyclic RGD pentapeptides
The synthesis and properties of Gla- and Phe-containing analogues of cyclic RGD pentapeptides
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DOI：
10.1039/b004677i
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发表时间：
2000-01-01
期刊：
影响因子：
--
通讯作者：
Naumer, C
中科院分区：
文献类型：
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作者：
Davies, JS;Enjalbal, C;Naumer, C
含有Arg-Gly-Asp基序的Cyclopentapeptides已经使用侧链保护的线性前体的固相组装，然后通过溶液相环化来合成。用γ-羧基谷氨酸（Gla）取代Asp残基是一种新的特征，其产生抑制细胞粘附的类似物，但其同系物在与重组整联蛋白受体的结合测定中不显示活性。NMR技术支持大多数类似物的β/γ-转角构象。
Cyclopentapeptides containing the Arg-Gly-Asp motif have been synthesised using solid-phase assembly of side-chain-protected linear precursors, followed by solution-phase cyclisation. The replacement of the Asp residue by gamma-carboxyglutamic acid (Gla) is a novel feature which gives rise to an analogue which inhibits cell adhesion, yet its congeners do not show activity in binding assays with recombinant integrin receptors. NMR techniques support a beta/gamma-turn conformation in most of the analogues.