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首页> 外文期刊>Bioorganic and Medicinal Chemistry Letters >Synthesis, characterization and anti-cancer activity of a peptide nucleolipid bioconjugate
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Synthesis, characterization and anti-cancer activity of a peptide nucleolipid bioconjugate

机译：肽核糖生物共轭物的合成，表征和抗癌活性

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The synthesis, characterization and anti-cancer activity of a novel peptide nucleolipid bioconjugate is reported in this study. The prerequisite 50-carboxy derived nucleolipid was synthesized following a five-step solution-phase approach and then coupled to the cytotoxic D-(KLAKLAK) 2 sequence by solid-phase bioconjugation. The biophysical and structural properties of the peptide-nucleolipid bioconjugate were evaluated and compared to the peptide controls. These characterization studies revealed that the amphiphilic peptides favored helical-type secondary structures and well-defined nanoparticle formulations that were found to be contributive towards their biological activity. The peptide-nucleolipid bioconjugate displayed greater lethality in comparison to the native D-(KLAKLAK)(2)AK sequence when treated within the human A549 non-small cell lung carcinoma cell line. Thus, the amphiphilic peptide-nucleolipid forms a new class of anti-cancer peptides that may be developed into promising leads in the fight against cancer. (C) 2016 Elsevier Ltd. All rights reserved.
机译：这项研究报道了新型肽核苷酸生物共轭物的合成，表征和抗癌活性。按照五步溶液相方法合成了必需的50-羧基衍生的核苷酸，然后通过固相生物缀合将其偶联到细胞毒性D-（KLAKLAK）2序列上。评估了肽-核苷酸生物缀合物的生物物理和结构特性，并将其与肽对照进行了比较。这些表征研究表明，两亲性肽偏爱螺旋型二级结构和定义明确的纳米颗粒制剂，这些制剂有助于它们的生物学活性。当在人A549非小细胞肺癌细胞系中治疗时，与天然D-（KLAKLAK）（2）AK序列相比，该肽-核苷酸生物缀合物显示出更大的杀伤力。因此，两亲性肽-核苷酸形成了一类新的抗癌肽，在对抗癌症中可以发展成为有希望的先导。 （C）2016 Elsevier Ltd.保留所有权利。

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