Genetically encoded fragment-based discovery from phage-displayed macrocyclic libraries with genetically encoded unnatural pharmacophores
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AI Ekanayake, L Sobze, P Kelich, J Youk…
Journal of the …, 2021
ACS Publications
Genetically encoded macrocyclic peptide libraries with unnatural pharmacophores are valuable sources for the discovery of ligands for many targets of interest. Traditionally, generation of such libraries employs “early stage” incorporation of unnatural building blocks into the chemically or translationally produced macrocycles. Here, we describe a divergent late-stage approach to such libraries starting from readily available starting material: genetically encoded libraries of peptides. A diketone linchpin 1, 5-dichloropentane-2, 4 …
