Plais Louise, Scheuermann Jörg
Department of Chemistry and Applied Biosciences, ETH Zürich (Swiss Federal Institute of Technology) Vladimir-Prelog-Weg 4 CH-8093 Zürich Switzerland
RSC Chem Biol. 2021 Oct 29;3(1):7-17. doi: 10.1039/d1cb00161b. eCollection 2022 Jan 5.
While macrocyclic peptides are extensively researched for therapeutically relevant protein targets, DNA-encoded chemical libraries (DELs) are developed at a quick pace to discover novel small molecule binders. The combination of both fields has been explored since 2004 and the number of macrocyclic peptide DELs is steadily increasing. Macrocycles with high affinity and potency were identified for diverse classes of proteins, revealing DEL's huge potential. By giving a historical perspective, we would like to review the methods which permitted the rise of macrocyclic peptide DELs, describe the different DELs which were created and discuss the achievements and challenges of this emerging field.
虽然大环肽针对与治疗相关的蛋白质靶点进行了广泛研究，但DNA编码化学文库（DELs）正快速发展以发现新型小分子结合剂。自2004年以来，这两个领域的结合已得到探索，且大环肽DELs的数量在稳步增加。针对各类蛋白质鉴定出了具有高亲和力和效力的大环化合物，揭示了DELs的巨大潜力。通过给出一个历史视角，我们希望回顾促使大环肽DELs兴起的方法，描述所创建的不同DELs，并讨论这一新兴领域的成就与挑战。
