Fig. 6. TRIB1 can potentially bind small-molecule ligands but not ATP.
(A and B) Representation of the available binding cavity of TRIB1 (gray) in (A) the SLE-out conformation from PDB ID 5CEM and (B) the SLE-in conformation when bound to C/EBPα. (C) DSF melting analysis of TRIB1 or TRIB1 + C/EBPα degron peptide in the presence or absence of ATP. Points are the mean of independent triplicates from one purified TRIB1 stock, with error bars representing SEM. (D) Summary of DSF analyses of TRIB1(84–372) against the Published Kinase Inhibitor Set (PKIS) library. Tm is expressed as the difference between each compound and the mean of three dimethyl sulfoxide (DMSO)–only controls. The four compounds shown in more detail in (E) are indicated. (E) Individual DSF melting curves of four selected compounds (left), with additional titrations for each that include C/EBPα degron peptide (right).