Phage-Assisted, Active Site-Directed Ligand Evolution with a Genetically Encoded Nε-Butyryl-ʟ-Lysine to Identify a Cellularly Potent and Selective Inhibitor for the ENL YEATS Domain as an Anti-Leukemia Agent
P.-H. C. Chen, X. S. Guo, H. E. Zhang, Z. Z. Geng, G. K. Dubey, C. A. Fierke, S. Xu, W. R. Liu
This study develops a phage-assisted ligand evolution method to identify potent ENL inhibitors, finding a pentapeptide with sub-nanomolar affinity and anti-leukemia activity.
bioRxiv · Jan 8, 2023 · PreprintBiochemistry