摘要
在过去几年中,将含金属分子与生物分子,特别是肽的特征相结合的兴趣已经增加。已经设计了大量新的创新有机金属化合物以及有效的配位络合物,特别是在药物化学中,生物活性化合物的文库通过引入金属络合物过度膨胀。研究的重点是潜水员,不限于例如, 开发具有抗增殖或抗菌活性的治疗剂,或用于制药应用的新型生物传感器的设计。通过引进金属中心,可能会增加新的特性,可以帮助克服疾病难以治理的问题,同时打击出现耐药性的问题。然而,许多非常有效的金属络合物的应用受到限制,因为它们的水溶性差,空气稳定性和与细胞接触时的较差的吸收。在这种情况下,优化有希望的铅结构的一种可能性是将其与生物活性肽偶联。在本综述中,介绍了用于药物设计和未来药物应用的金属络合物 - 肽缀合物的概述。
关键词: 细胞穿透肽,抗菌肽,固相肽合成,有机金属配合物,抗癌治疗,生物传感器。
Current Medicinal Chemistry
Title:Metal Complex-Peptide Conjugates: How to Modulate Bioactivity of Metal-Containing Compounds by the Attachment to Peptides
Volume: 24 Issue: 17
关键词: 细胞穿透肽,抗菌肽,固相肽合成,有机金属配合物,抗癌治疗,生物传感器。
摘要: During the last years, the interest in combining the features of metal-containing molecules with biomolecules, particularly peptides, has been increased. Large series of new innovative organometallic compounds, as well as potent coordination complexes have been designed and, especially in medicinal chemistry, the library of bioactive compounds was excessively expanded by the introduction of metal complexes. The research foci are divers and not limited to e.g. the development of therapeutics with anti-proliferative or antibacterial activity, or the design of novel biosensors useful for pharmaceutical applications. By introduction of a metal centre, new attributes might be added that could help to overcome the problems of difficult to treat diseases, as well as to combat issues with arising drug resistances. However, the application of a number of very potent metal complexes is restricted owing to their poor water-solubility, air-stability and only poor uptake when in contact with cells. In this context, one possibility to optimize promising lead structures is to couple them to bioactive peptides. Within this review, an overview on metal complex-peptide conjugates used for drug design and future pharmaceutical application is presented.
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Cite this article as:
Metal Complex-Peptide Conjugates: How to Modulate Bioactivity of Metal-Containing Compounds by the Attachment to Peptides, Current Medicinal Chemistry 2017; 24 (17) . https://dx.doi.org/10.2174/0929867324666170505112836
DOI https://dx.doi.org/10.2174/0929867324666170505112836 |
Print ISSN 0929-8673 |
Publisher Name Bentham Science Publisher |
Online ISSN 1875-533X |
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