Dathe M, Wieprecht T
Research Institute of Molecular Pharmacology, Alfred-Kowalke-Strasse 4, D-10315, Berlin, Germany.
Biochim Biophys Acta. 1999 Dec 15;1462(1-2):71-87. doi: 10.1016/s0005-2736(99)00201-1.
Antibacterial, membrane-lytic peptides belong to the innate immune system and host defense mechanism of a multitude of animals and plants. The largest group of peptide antibiotics comprises peptides which fold into an amphipathic alpha-helical conformation when interacting with the target. The activity of these peptides is thought to be determined by global structural parameters rather than by the specific amino acid sequence. This review is concerned with the influence of structural parameters, such as peptide helicity, hydrophobicity, hydrophobic moment, peptide charge and the size of the hydrophobic/hydrophilic domain, on membrane activity and selectivity. The potential of these parameters to increase the antibacterial activity and to improve the prokaryotic selectivity of natural and model peptides is assessed. Furthermore, biophysical studies are summarized which elucidated the molecular basis for activity and selectivity modulations on the level of model membranes. Finally, the knowledge about the role of peptide structural parameters is applied to understand the different activity spectra of natural membrane-lytic peptides.
抗菌性膜溶解肽属于众多动植物的先天免疫系统和宿主防御机制。最大的一类肽抗生素包括与靶标相互作用时折叠成两亲性α-螺旋构象的肽。这些肽的活性被认为是由整体结构参数而非特定氨基酸序列决定的。本综述关注结构参数,如肽的螺旋度、疏水性、疏水矩、肽电荷以及疏水/亲水区的大小对膜活性和选择性的影响。评估了这些参数提高天然肽和模型肽抗菌活性以及改善原核选择性的潜力。此外,总结了阐明模型膜水平上活性和选择性调节分子基础的生物物理研究。最后,运用关于肽结构参数作用的知识来理解天然膜溶解肽的不同活性谱。