Phage-Assisted, Active Site-Directed Ligand Evolution of a Potent and Selective Histone Deacetylase 8 Inhibitor
J. S. Morse, Y. J. Sheng, J. T. Hampton, L. D. Sylvain, S. Das, Y. R. Alugubelli, P.-H. C. Chen, K. S. Yang, S. Xu, C. A. Fierke, W. R. Liu
This paper develops PADLE, a phage-assisted method to evolve potent HDAC8 inhibitors, identifying two highly selective and potent inhibitors with sub-nanomolar Ki values.
bioRxiv · Sep 14, 2022Biochemistry