Intracellular trapping of the selective phosphoglycerate dehydrogenase (PHGDH) inhibitor BI-4924 disrupts serine biosynthesis

Weinstabl H, Treu M, Rinnenthal J, Zahn SK, Ettmayer P, Bader G, Dahmann G, Kessler D, Rumpel K, Mischerikow N, Savarese F, Gerstberger T, Mayer M, Zoephel A, Schnitzer R, Sommergruber W, Martinelli P, Arnhof H, Peric-Simov B, Hofbauer KS, Garavel G, Scherbantin Y, Mitzner S, Fett TN, Scholz G, Bruchhaus J, Burkard M, Kousek R, Ciftci T, Sharps B, Schrenk A, Harrer C, Haering D, Wolkerstorfer B, Zhang X, Lv X, Du A, Li D, Li Y, Quant J, Pearson M & McConnell DB
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Weinstabl, H., Treu, M., Rinnenthal, J., Zahn, S. K., Ettmayer, P., Bader, G., … McConnell, D. B. (2019). Intracellular trapping of the selective phosphoglycerate dehydrogenase (PHGDH) inhibitor BI-4924 disrupts serine biosynthesis. Journal of Medicinal Chemistry, 62(17), 7976-7997. https://doi.org/10.1021/acs.jmedchem.9b00718