Discovery and optimization of piperazine-1-thiourea-based human phosphoglycerate dehydrogenase inhibitors
J. M. Rohde, K. R. Brimacombe, L. Liu, M. E. Pacold, A. Yasgar, D. M. Cheff, T. D. Lee, G. Rai, B. Baljinnyam, Z. Li, A. Simeonov, M. D. Hall, M. Shen, D. M. Sabatini, M. B. Boxer
The paper develops a biochemical assay to screen for PHGDH inhibitors, identifies piperazine-1-thiourea compounds, and evaluates their biological impact on serine metabolism in cancer cells.
Bioorganic & Medicinal Chemistry · May 1, 2018Peer-reviewedCancer Biology