6E37

O-GlcNAc Transferase in complex with covalent inhibitor

Summary for 6E37

• Entry DOI: 10.2210/pdb6e37/pdb
• Descriptor: O-GlcNAc transferase subunit p110, TYR-PRO-GLY-GLY-SER-THR-PRO-VAL-SER-SER-ALA-ASN, (2S,3R,4R,5S,6R)-3-[(2E)-but-2-enoylamino]-4,5-dihydroxy-6-(hydroxymethyl)tetrahydro-2H-thiopyran-2-yl [(2R,3S,4R,5R)-5-(2,4-dioxo-3,4-dihydropyrimidin-1(2H)-yl)-3,4-dihydroxytetrahydrofuran-2-yl]methyl dihydrogen diphosphate (non-preferred name), ... (4 entities in total)
• Functional Keywords: o-glcnac transferase, inhibitor, transferase-inhibitor complex, transferase/inhibitor
• Biological source: Homo sapiens (Human); More
• Total number of polymer chains: 2
• Total formula weight: 83022.53

Authors

Li, H.,Jiang, J. (deposition date: 2018-07-13, release date: 2019-11-06, Last modification date: 2024-10-16)

Primary citation

Worth, M.,Hu, C.W.,Li, H.,Fan, D.,Estevez, A.,Zhu, D.,Wang, A.,Jiang, J.
Targeted covalent inhibition of O-GlcNAc transferase in cells.
Chem.Commun.(Camb.), 55:13291-13294, 2019

PubMed Abstract: O-GlcNAc transferase (OGT) glycosylates numerous proteins and is implicated in many diseases. To date, most OGT inhibitors lack either sufficient potency or characterized specificity in cells. We report the first targeted covalent inhibitor that predominantly reacts with OGT but does not affect other functionally similar enzymes. This study provides a new strategy to interrogate cellular OGT functions and to investigate other glycosyltransferases.

PubMed: 31626249
DOI: 10.1039/c9cc04560k

Experimental method

X-RAY DIFFRACTION (2.531 Å)