Discovery and pharmacological characterization of a new class of prolyl-tRNA synthetase inhibitor for anti-fibrosis therapy
Fig 1
T-3833261 is a potent ATP competitive PRS inhibitor.
(A) Molecular model constructed by available PRS crystal structures bearing adenosine and proline (PDB: 4K87) and Halofuginone (PDB: 4K88), (B) Binding mode of T-3833261 in the ATP binding site, (C) Chemical structure, (D) Biochemical activity of compound in PRS inhibition measured by an ATP/PPi exchange method. Results performed in duplicate are shown as the mean ± SD. The inhibitory activities are expressed as the percentage of vehicle-treated control.