中文摘要：在许多适合用于治疗的分子实体中，肽是药物学术发现和开发的不错选择。其模块化结构和可扩展性、功能强大且价格合理的筛选平台的可用性以及合成相对容易，使得治疗性肽易用于教学和研究。巴塞尔大学分子制药集团高度关注包括补体和肾素-血管紧张素系统在内的宿主防御途径的治疗调节，主要通过肽向学生介绍现代药物设计，以发现免疫和炎症疾病的新疗法，并扩大有前景的药物类别的临床前开发。目前研究涉及从学生驱动的肽型血管紧张素转换酶抑制剂的迭代设计和利用噬菌体展示技术发现新的免疫调节剂，到生物材料和移植用保护性肽涂层的开发，以及结构-活性关系指导的后期临床试验候选治疗肽药物优化。即使在当前阶段，肽也可以在药物研究和教育之间实现完美的循环，而肽类药物临床应用的最新进展可能只会增加这一多功能药物类别的价值和相关性。
外文摘要：Among the many molecular entities suitable for therapeutic use, peptides have emerged as a particularly attractive option for academic drug discovery and development. Their modular structure and extendibility, the availability of powerful and affordable screening platforms, and the relative ease-of-synthesis render therapeutic peptides highly approachable for teaching and research alike. With a strong focus on the therapeutic modulation of host defence pathways, including the complement and renin-angiotensin systems, the Molecular Pharmacy group at the University of Basel strongly relies on peptides to introduce students to practical aspects of modern drug design, to discover novel therapeutics for immune and inflammatory diseases, and to expand on options for the preclinical development of a promising drug class. Current projects reach from student-driven iterative design of peptidic angiotensin-converting enzyme inhibitors and the use of phage display technology to discover novel immune modulators to the development of protective peptide coatings for biomaterials and transplants and the structure-activity-relationship-guided optimization of therapeutic peptide drug candidates in late-stage clinical trials. Even at the current stage, peptides allow for a perfect circle between pharmaceutical research and education, and the recent spark of clinical applications for peptide-based drugs may only increase the value and relevance of this versatile drug class.
外文关键词：ACE inhibitors；Complement；Host defence；Phage display；Peptide therapeutics
作者：Schwardt, O；Lamers, C；Bechtler, C；Ricklin, D
作者单位：Univ Basel
期刊名称：CHIMIA
期刊影响因子：1.478
出版年份：2021
出版刊次：6
点击下载：治疗性肽能恢复被误导的宿主防御和体内平衡：从教学到概念到临床