School of Pharmacy and Biomolecular Sciences, Faculty of Science, Liverpool John Moores University, Liverpool L3 3AF, UK.
Institute of Chemical Sciences, School of Engineering and Physical Sciences, Heriot-Watt University, Edinburgh EH14 4AS, UK.
Drug Discov Today. 2021 Jun;26(6):1409-1419. doi: 10.1016/j.drudis.2021.02.019. Epub 2021 Feb 26.
As of 2020, there were >100 approved peptides with therapeutic or diagnostic applications. However, a complete database providing information on marketed peptides is not freely available, making the peptide chemists' job of designing future peptide drug candidates challenging. Unlike the rules for small-molecule drugs, there is no general set of guidelines for designing a successful peptide-based drug. In this review, together with our freely available database (PepTherDia, http://peptherdia.herokuapp.com), we provide insights into what a successful peptide therapeutic or diagnostic agent looks like and lay the foundation for establishing a set of rules to help future medicinal chemists to design peptide candidates with increased approval rates.
截至 2020 年,已有超过 100 种经过批准的具有治疗或诊断应用的肽。然而,一个提供有关市售肽信息的完整数据库并不免费提供,这使得设计未来肽类药物候选物的肽化学家的工作具有挑战性。与小分子药物的规则不同,设计成功的基于肽的药物没有一套通用的指导方针。在这篇综述中,我们结合我们免费提供的数据库(PepTherDia,http://peptherdia.herokuapp.com),深入了解成功的肽治疗或诊断剂的外观,并为建立一套规则奠定基础,以帮助未来的药物化学家设计批准率更高的肽候选物。