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Front Cover: Toward Angiogenesis Inhibitors Based on the Conjugation of Organometallic Platinum(II) Complexes to RGD Peptides (ChemMedChem 17/2018)
ChemMedChem ( IF 3.4 ) Pub Date : 2018-09-03 , DOI: 10.1002/cmdc.201800570
Ana Zamora 1, 2 , Albert Gandioso 1 , Anna Massaguer 3 , Silvia Buenestado 4 , Carme Calvis 4 , Jose Luis Hernández 4 , Francesc Mitjans 4 , Venancio Rodríguez 2 , José Ruiz 2 , Vicente Marchán 1
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The Front Cover illustrates the ability of a nontoxic conjugate between a cyclometalated platinum(II) complex and a cyclic peptide containing the RGD sequence (‐Arg‐Gly‐Asp‐) to induce morphological changes and cell detachment of αVβ3‐overexpressing SK‐MEL‐28 cancer cells. This conjugate shows a similar angiogenesis pattern of activity to that of reference peptide Cilengitide at subcytotoxic concentrations in HUVEC cells. This result opens the way to target tumor vasculature through the development of a novel class of angiogenesis inhibitors based on the conjugation of compounds with high antiangiogenic activity, such as metal complexes or small organic molecules, to cyclic RGD‐containing peptides or peptidomimetic analogues. More information can be found in the Full Paper by José Ruiz, Vicente Marchán et al. on page 1755 in Issue 17, 2018 (DOI: 10.1002/cmdc.201800282).
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中文翻译:

封面:基于有机金属铂(II)配合物与RGD肽结合的血管生成抑制剂(ChemMedChem 17/2018)

前盖示出了无毒性缀合物的环金属铂之间的能力(II)络合物和含有RGD序列(-Arg酰-Gly-Asp-的)来诱导形态学变化和α的细胞剥离的环肽V β 3过度表达SK‐MEL‐28癌细胞。该缀合物在HUVEC细胞中的亚细胞毒性浓度下显示出与参考肽西仑吉肽相似的血管生成活性。这一结果为新型血管生成抑制剂的开发开辟了靶向肿瘤脉管系统的途径,该抑制剂基于具有高抗血管生成活性的化合物(例如金属络合物或小的有机分子)与含环状RGD的肽或拟肽类似物的缀合。有关更多信息,请参见何塞·鲁伊斯(JoséRuiz),维森特·马尚(VicenteMarchán)等人的论文。就在第17期,2018页1755(:10.1002 / cmdc.201800282 DOI)。
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更新日期:2018-09-03
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