Fig. 4: Chelerythrine is a yCPT1 inhibitor. | Nature Communications

Fig. 4: Chelerythrine is a yCPT1 inhibitor.

From: Structural basis for catalysis and selectivity of phospholipid synthesis by eukaryotic choline-phosphotransferase

Fig. 4

a Titration of chelerythrine for the inhibition of yCPT1 WT. The level of CMP released from CDP-choline was evaluated in the presence of chelerythrine at the indicated concentration. Data are presented as the mean ± SD from three independent measurements. b, c 3.2 Å resolution cryo-EM density map and model of yCPT1 dimer bound to chelerythrine. Density and model are depicted and colored in the same way as shown in Fig. 1: yellow, catalytic domain; purple, CDP-AP signature motif; gray, dimerization domain; brown, N-terminal stretch; cyan, phosphatidylcholine (PC). Chelerythrine is colored pale green. d The chelerythrine-binding pocket in yCPT1 is enlarged with chelerythrine and surrounding residues shown as a stick models. e LigPlot2 is used for the analysis of the chelerythrine-binding pocket and the illustration. Source data are provided as a Source Data file.

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