Tapeinou Anthi, Matsoukas Minos-Timotheos, Simal Carmen, Tselios Theodore
Department of Chemistry, University of Patras, 26500, Patras, Greece.
Department of Biostatistics, Laboratory of Computational Medicine, Autonomous University of Barcelona, 08193, Bellaterra, Spain.
Biopolymers. 2015 Sep;104(5):453-61. doi: 10.1002/bip.22669.
Peptides and proteins are attractive initial leads for the rational design of bioactive molecules. Several natural cyclic peptides have recently emerged as templates for drug design due to their resistance to chemical or enzymatic hydrolysis and high selectivity to receptors. The development of practical protocols that mimic the power of nature's strategies remains paramount for the advancement of novel peptide-based drugs. The de novo design of peptide mimetics (nonpeptide molecules or cyclic peptides) for the synthesis of linear or cyclic peptides has enhanced the progress of therapeutics and diverse areas of science and technology. In the case of metabolically unstable peptide ligands, the rational design and synthesis of cyclic peptide analogues has turned into an alternative approach for improved biological activity.
肽和蛋白质是生物活性分子合理设计中具有吸引力的初始先导物。最近，几种天然环肽因其对化学或酶促水解的抗性以及对受体的高选择性而成为药物设计的模板。开发模仿自然策略威力的实用方案对于新型肽基药物的发展仍然至关重要。用于合成线性或环肽的肽模拟物（非肽分子或环肽）的从头设计促进了治疗学以及科学技术各个领域的进步。对于代谢不稳定的肽配体，环肽类似物的合理设计和合成已成为提高生物活性的替代方法。
