Structures of Trypanosoma brucei Methionyl-tRNA Synthetase with Urea-Based Inhibitors Provide Guidance for Drug Design against Sleeping Sickness

• Main Authors: Koh C.Y., Kim J.E., Wetzel A.B., de van der Schueren W.J., Shibata S., Ranade R.M., Liu J., Zhang Z., Gillespie J.R., Buckner F.S., Verlinde C.L.M.J., Fan E., Hol W.G.J.
• Other Authors: MEDICINE
• Format: Article
• Published: 2019
• Subjects: adenosine triphosphate; aminoquinolone based inhibitor; antitrypanosomal agent; enzyme inhibitor; methionine transfer RNA ligase; unclassified drug; urea based inhibitor; African trypanosomiasis; aminoacylation; article; crystal structure; drug design; drug targeting; high performance liquid chromatography; IC 50; ligand binding; mass spectrometry; membrane permeability; nuclear magnetic resonance spectroscopy; protein expression; protein interaction; protein purification; protein structure; site directed mutagenesis; synthesis; Trypanosoma brucei; Antiprotozoal Agents; Binding Sites; Crystallography, X-Ray; Drug Design; Enzyme Inhibitors; Humans; Inhibitory Concentration 50; Methionine-tRNA Ligase; Models, Molecular; Parasitic Sensitivity Tests; Protein Conformation; Trypanosoma brucei brucei; Urea
• Online Access: https://scholarbank.nus.edu.sg/handle/10635/161610
• Institution: National University of Singapore

10.1371/journal.pntd.0002775