Projects per year
Abstract
Inhibitors of OGT (O-GlcNAc transferase) are valuable tools to study the cell biology of protein O-GlcNAcylation. We report OGT bisubstrate-linked inhibitors (goblins) in which the acceptor serine in the peptide VTPVSTA is covalently linked to UDP, eliminating the GlcNAc pyranoside ring. Goblin1 co-crystallizes with OGT, revealing an ordered C3 linker and retained substrate-binding modes, and binds the enzyme with micromolar affinity, inhibiting glycosyltransfer on to protein and peptide substrates.
Original language | English |
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Pages (from-to) | 497-502 |
Number of pages | 6 |
Journal | Biochemical Journal |
Volume | 457 |
Issue number | 3 |
DOIs | |
Publication status | Published - 1 Feb 2014 |
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Dive into the research topics of 'Bisubstrate UDP-peptide conjugates as human O-GlcNAc transferase inhibitors'. Together they form a unique fingerprint.Projects
- 2 Finished
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Aref#d: 21559. Molecular Mechanisms of Fungal Cell Wall Assembly (Programme Grant)
van Aalten, D. (Investigator)
1/11/09 → 31/10/14
Project: Research
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Aref#d: 21318. Molecular Mechanisms of O-GlcNAc Signalling (Senior Fellowship Renewal)
van Aalten, D. (Investigator)
1/06/09 → 29/02/16
Project: Research
Student theses
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Developing O-GlcNAc transferase inhibitors - insights from substrate recognition
Rafie, K. (Author), van Aalten, D. (Supervisor), 2017Student thesis: Doctoral Thesis › Doctor of Philosophy
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Understanding tetratricopeptide repeats of O-GlcNAc transferase
Gundogdu, M. (Author), van Aalten, D. (Supervisor), 2017Student thesis: Doctoral Thesis › Doctor of Philosophy
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