Neundorf Ines
Department of Chemistry, Institute of Biochemistry, University of Cologne, Cologne, Germany.
Curr Med Chem. 2017;24(17):1853-1861. doi: 10.2174/0929867324666170505112836.
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.
在过去几年中,将含金属分子与生物分子(特别是肽)的特性相结合的研究兴趣有所增加。已经设计了大量新型创新有机金属化合物以及强效配位络合物,尤其是在药物化学领域,通过引入金属络合物,生物活性化合物库得到了极大扩展。研究重点多种多样,不限于例如开发具有抗增殖或抗菌活性的治疗剂,或设计用于药物应用的新型生物传感器。通过引入金属中心,可能会增加新的特性,有助于克服难以治疗疾病的问题,以及应对出现的耐药性问题。然而,许多非常强效的金属络合物的应用受到限制,这是由于它们的水溶性差、空气稳定性差以及与细胞接触时摄取性不佳。在这种情况下,优化有前景的先导结构的一种可能性是将它们与生物活性肽偶联。在本综述中,对用于药物设计和未来药物应用的金属络合物 - 肽缀合物进行了概述。