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首页> 外文期刊>Chemistry: A European journal >Cyclic isoDGR and RGD Peptidomimetics Containing Bifunctional Diketopiperazine Scaffolds are Integrin Antagonists
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Cyclic isoDGR and RGD Peptidomimetics Containing Bifunctional Diketopiperazine Scaffolds are Integrin Antagonists

机译：包含双功能二酮哌嗪支架的环状isoDGR和RGD拟肽是整合素拮抗剂。

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摘要

The cyclo[DKP-isoDGR] peptidomimetics 2-5, containing bifunctional diketopiperazine (DKP) scaffolds that differ in the configuration of the two DKP stereocenters and in the substitution at the DKP nitrogen atoms, were prepared and examined in vitro in competitive binding assays with purified (v3) and (v5) integrin receptors. IC50 values ranged from low nanomolar (ligand 3) to submicromolar with (v3) integrin. The biological activities of ligands cyclo[DKP3-RGD] 1 and cyclo[DKP3-isoDGR] 3, bearing the same bifunctional DKP scaffold and showing similar (V3) integrin binding values, were compared in terms of their cellular effects in human U373 glioblastoma cells. Compounds 1 and 3 displayed overlapping inhibitory effects on the FAK/Akt integrin activated transduction pathway and on integrin-mediated cell infiltration processes, and qualify therefore, despite the different RGD and isoDGR sequences, as integrin antagonists. Both compounds induced apoptosis in glioma cells after 72hour treatment.
机译：制备了环[DKP-isoDGR]拟肽2-5，其中包含在两个DKP立体中心的构型以及DKP氮原子的取代方面不同的双功能二酮哌嗪（DKP）支架，并在体外进行了竞争性结合测定纯化（v3）和（v5）整合素受体。 IC50值范围从低纳摩尔（配体3）到亚微摩尔（v3）整联蛋白。根据在人U373胶质母细胞瘤细胞中的细胞效应，比较了具有相同双功能DKP支架并显示相似（V3）整联蛋白结合值的配体cyclo [DKP3-RGD] 1和cyclo [DKP3-isoDGR] 3的生物活性。 。化合物1和3对FAK / Akt整合素激活的传导途径和整合素介导的细胞浸润过程显示出重叠的抑制作用，因此尽管有不同的RGD和isoDGR序列，但它们仍可作为整合素拮抗剂。治疗72小时后，这两种化合物均诱导神经胶质瘤细胞凋亡。

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