Structure-Based Evolution of Low Nanomolar O‑GlcNAc Transferase Inhibitors

• Published in: Journal of the American Chemical Society Vol. 140; no. 42; pp. 13542 - 13545
• Main Authors: Martin, Sara E. S, Tan, Zhi-Wei, Itkonen, Harri M, Duveau, Damien Y, Paulo, Joao A, Janetzko, John, Boutz, Paul L, Törk, Lisa, Moss, Frederick A, Thomas, Craig J, Gygi, Steven P, Lazarus, Michael B, Walker, Suzanne
• Format: Journal Article
• Language: English
• Published: United States American Chemical Society 24.10.2018; American Chemical Society (ACS)
• Subjects: Animalia; enzyme inhibition; enzyme inhibitors; glycosylation; glycosyltransferases; N-acetylglucosamine; proteins

Reversible glycosylation of nuclear and cytoplasmic proteins is an important regulatory mechanism across metazoans. One enzyme, O-linked N-acetylglucosamine transferase (OGT), is responsible for all nucleocytoplasmic glycosylation and there is a well-known need for potent, cell-permeable inhibitors...