Walker, Suzanne (Harvard University)
Martin Schwanger, Sara (Harvard University)
Thomas, Craig (NCATS)
Duveau, Damien (NCATS)
This technology includes the development and use of small molecules that inhibit O-linked beta-N-acetylglucosamine (O-GlcNAc) transferase (OGT) for a variety of pathologies, including Alzheimer's disease, cancer, cancer, diabetes, and neurodegenerative disorders the treatment of cancer and as a potential antiviral. OGT is a ubiquitous enzyme that catalyzes the transfer of N-acetylglucosamine (GlcNAc) to the serine or threonine residues of nuclear and cytoplasmic proteins. The addition of GlcNAc to proteins is a similar post-translational modification as phosphorylation and has been described to occur thousands of proteins.
Further work with O-linked beta-N-acetylglucosamine transferase (OGT) inhibitors will permit the further study of the biological role of OGT in cell homeostasis. Further clinical work could establish OGT inhibitors, alone or in combination with other agents, for the treatment of several disorders including cancer and as an antiviral.
The series of O-linked beta-N-acetylglucosamine transferase (OGT) inhibitors described in this technology exhibit improved binding properties and OGT inhibition.