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Peptides derived from the histidine–proline rich glycoprotein bind copper ions and exhibit anti-angiogenic properties†
Dalton Transactions ( IF 3.5 ) Pub Date : 2018-06-20 00:00:00 , DOI: 10.1039/c8dt01560k Antonio Magrì 1, 2, 3 , Giulia Grasso 1, 2, 3 , Federico Corti 4, 5, 6, 7 , Federica Finetti 3, 8, 9, 10, 11 , Valentina Greco 3, 12, 13, 14 , Anna Maria Santoro 1, 2, 3 , Sebastiano Sciuto 3, 12, 13, 14 , Diego La Mendola 3, 15, 16, 17 , Lucia Morbidelli 3, 10, 11, 18 , Enrico Rizzarelli 3, 12, 13, 14
Dalton Transactions ( IF 3.5 ) Pub Date : 2018-06-20 00:00:00 , DOI: 10.1039/c8dt01560k Antonio Magrì 1, 2, 3 , Giulia Grasso 1, 2, 3 , Federico Corti 4, 5, 6, 7 , Federica Finetti 3, 8, 9, 10, 11 , Valentina Greco 3, 12, 13, 14 , Anna Maria Santoro 1, 2, 3 , Sebastiano Sciuto 3, 12, 13, 14 , Diego La Mendola 3, 15, 16, 17 , Lucia Morbidelli 3, 10, 11, 18 , Enrico Rizzarelli 3, 12, 13, 14
Affiliation
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The role of copper in cancer progression has been established since decades. Additionally, copper is able to stimulate angiogenesis through the control of VEGF expression and activity in endothelial cells. In this paper a tetrapeptide, belonging to the histidine–proline-rich glycoprotein (HPRG) and encompassing four repeats of the sequence GHHPH (named TetraHPRG), was synthesized and its copper(II) complex species were characterized by means of potentiometry, UV-vis, circular dichroism (CD), electron paramagnetic resonance (EPR) and electron spray ionization mass spectrometry (ESI-MS). Moreover, a peptide covalently bound through an amidic bond to trehalose (TH-TetraHPRG) was designed and synthesized as a prodrug system. The activity of both TetraHPRG and TH-TetraHPRG molecules on copper and VEGF induced angiogenic responses in endothelial cells was assessed. The two peptides show a similar and effective anti-angiogenic activity on both molecular and cellular responses. Since the trehalose derivative has a higher resistance to enzymatic degradation, it can be further exploited as a potential drug delivery system with anti-angiogenic activity.
中文翻译：
源自富含组氨酸-脯氨酸的糖蛋白的肽结合铜离子并显示出抗血管生成特性†
数十年来，铜在癌症进展中的作用已经确立。另外，铜能够通过控制内皮细胞中的VEGF表达和活性来刺激血管生成。本文合成了一种四肽，它属于富含组氨酸-脯氨酸的糖蛋白（HPRG），它包含GHHPH序列的四个重复序列（称为TetraHPRG），其铜离子（II）通过电位计，紫外可见光谱，圆二色性（CD），电子顺磁共振（EPR）和电子喷雾电离质谱（ESI-MS）对复杂的物种进行表征。此外，设计并合成了通过酰胺键与海藻糖共价结合的肽（TH-TetraHPRG），并将其合成为前药系统。评估了TetraHPRG和TH-TetraHPRG分子对铜和VEGF诱导的内皮细胞血管生成反应的活性。这两种肽对分子和细胞反应均显示出相似且有效的抗血管生成活性。由于海藻糖衍生物对酶促降解具有更高的抗性，因此它可以被进一步开发为具有抗血管生成活性的潜在药物递送系统。
更新日期：2018-06-20
中文翻译：
源自富含组氨酸-脯氨酸的糖蛋白的肽结合铜离子并显示出抗血管生成特性†
数十年来，铜在癌症进展中的作用已经确立。另外，铜能够通过控制内皮细胞中的VEGF表达和活性来刺激血管生成。本文合成了一种四肽，它属于富含组氨酸-脯氨酸的糖蛋白（HPRG），它包含GHHPH序列的四个重复序列（称为TetraHPRG），其铜离子（II）通过电位计，紫外可见光谱，圆二色性（CD），电子顺磁共振（EPR）和电子喷雾电离质谱（ESI-MS）对复杂的物种进行表征。此外，设计并合成了通过酰胺键与海藻糖共价结合的肽（TH-TetraHPRG），并将其合成为前药系统。评估了TetraHPRG和TH-TetraHPRG分子对铜和VEGF诱导的内皮细胞血管生成反应的活性。这两种肽对分子和细胞反应均显示出相似且有效的抗血管生成活性。由于海藻糖衍生物对酶促降解具有更高的抗性，因此它可以被进一步开发为具有抗血管生成活性的潜在药物递送系统。
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