Constrained Peptides in Drug Discovery and Development
Constrained Peptides in Drug Discovery and Development
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DOI：
10.5059/yukigoseikyokaishi.75.1171
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发表时间：
2017-11-01
影响因子：
0.2
通讯作者：
Masuya, Keiichi
中科院分区：
文献类型：
--
作者：
Cary, Douglas R.;Ohuchi, Masaki;Masuya, Keiichi
约束肽，即大环肽和钉合肽，作为一类有前途的抑制蛋白质-蛋白质相互作用（PPI）的化合物正受到越来越多的关注。讨论了肽疗法的现状，包括其优点和挑战，以及开启肽研究和开发新时代的最新技术发展。描述了PeptiDream的肽发现平台系统（PDPS）背后的技术，展示了它如何用于快速生成受限肽库并获得详细的SAR信息。该技术可以以很高的成功率提供有效的肽配体，这些配体本身可以开发为候选药物，用于肽药物缀合物（PDC）或转化为小分子药物先导物。约束肽及其在临床中的应用领域的前景也进行了描述。
Constrained peptides, namely macrocyclic and stapled peptides, are receiving increasing attention as a promising class of compounds for the inhibition of protein-protein interactions (PPI). The current state of peptide therapeutics is discussed, including their merits and challenges, as well as recent technological developments that have enabled a new era in peptide research and development. The technology behind PeptiDream's Peptide Discovery Platform System (PDPS) is described, showing how it can be used to rapidly generate libraries of constrained peptides and obtain detailed SAR information. This technology can provide, with a high rate of success, potent peptide ligands that may be developed as drug candidates themselves, utilized in peptide drug conjugates (PDC), or converted into small molecule drug leads. The outlook for the field of constrained peptides and their use in the clinic is also described.