Fig. 4: DLPTP reveals LAP3 as a target of PCI-34051 and BRD-3811. | Nature Communications

Fig. 4: DLPTP reveals LAP3 as a target of PCI-34051 and BRD-3811.

From: A computational method for detection of ligand-binding proteins from dose range thermal proteome profiles

Fig. 4: DLPTP reveals LAP3 as a target of PCI-34051 and BRD-3811.

a Chemical structure of the HDAC8 inhibitor PCI-34051. b Volcano plot of the 2D-TPP experiment with PCI-34051 in HL-60 cells. c Chemical structure of BRD-3811, an analog of PCI-34051 in which the Zn2+ chelating hydroxamic acid (HA) group is sterically hindered by a methyl group (highlighted in red). d Volcano plot of the 2D-TPP experiment with BRD-3811 in HL-60 cells. e Fluorescence intensity measured over time in a fluorometric leucine aminopeptidase assay with recombinant LAP3 in the presence of PCI-34051, BRD-3811, or vehicle control. Axes in b and d are outlined in Fig. 1b.

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