Thursday, August 11, 2016

Characterization of Novel Small-Molecule NRF2 Activators: Structural and Biochemical Validation of Stereospecific KEAP1 Binding

Carlos Huerta, Xin Jiang, Isaac Trevino, Christopher F. Bender, Deborah A. Ferguson, Brandon Probst, Kerren K. Swinger, Vincent S. Stoll, Philip J. Thomas, Irina Dulubova, Melean Visnick, W. Christian Wigley, Biochimica et Biophysica Acta (BBA) - General Subjects, Available online 27 July 2016, ISSN 0304-4165, doi:10.1016/j.bbagen.2016.07.026.

Clinical trials of omaveloxolone are currently underway in several indications, including Friedreich’s Ataxia, mitochondrial myopathies, corneal endothelial cell loss following cataract surgery, and melanoma. The increased risk for acute fluid overload adverse events observed in BEACON with late-stage CKD patients has not been observed in subsequent studies with bardoxolone methyl or omaveloxolone.