Overview of the assays to probe O-linked β-N-acetylglucosamine transferase binding and activity

Balsollier, Cyril (avtor), Pieters, Roland J. (avtor), Anderluh, Marko (avtor)

O-GlcNAcylation is a posttranslational modification that occurs at serine and threonine residues of protein substrates by the addition of O-linked β-D-N-acetylglucosamine (GlcNAc) moiety. Two enzymes are involved in this modification: O-GlcNac transferase (OGT), which attaches the GlcNAc residue to the protein substrate, and O-GlcNAcase (OGA), which removes it. This biological balance is important for many biological processes, such as protein expression, cell apoptosis, and regulation of enzyme activity. The extent of this modification has sparked interest in the medical community to explore OGA and OGT as therapeutic targets, particularly in degenerative diseases. While some OGA inhibitors are already in phase 1 clinical trials for the treatment of Alzheimer’s disease, OGT inhibitors still have a long way to go. Due to complex expression and instability, the discovery of potent OGT inhibitors is challenging. Over the years, the field has grappled with this problem, and scientists have developed a number of techniques and assays. In this review, we aim to highlight assays and techniques for OGT inhibitor discovery, evaluate their strength for the field, and give us direction for future bioassay methods.

• Jezik: Angleški jezik
• Ključne besede: OGT, GlcNAcylation, O-GlcNAc transferase, bioassay, OGT inhibitor
• Vrsta gradiva: Članek v reviji
• Tipologija: 1.02 - Pregledni znanstveni članek
• Organizacija: FFA - Fakulteta za farmacijo
• Status publikacije: Objavljeno
• Različica publikacije: Objavljena publikacija
• Leto izida: 2021
• Št. strani: 20 str.
• Številčenje: Vol. 26, iss. 4, art. 1037
• PID: 20.500.12556/RUL-135020
• UDK: 615.4:54:616.894
• ISSN pri članku: 1420-3049
• DOI: 10.3390/molecules26041037
• COBISS.SI-ID: 51829507
• Datum objave v RUL: 17.02.2022

Gradivo je del revije

• Naslov: Molecules
• Skrajšan naslov: Molecules
• Založnik: MDPI
• ISSN: 1420-3049
• COBISS.SI-ID: 18462981

Licence

• Licenca: CC BY 4.0, Creative Commons Priznanje avtorstva 4.0 Mednarodna
• Povezava: http://creativecommons.org/licenses/by/4.0/deed.sl
• Opis: To je standardna licenca Creative Commons, ki daje uporabnikom največ možnosti za nadaljnjo uporabo dela, pri čemer morajo navesti avtorja.
• Začetek licenciranja: 16.02.2021

Sekundarni jezik

• Jezik: Slovenski jezik
• Ključne besede: farmacevtska kemija, Alzheimerjeva bolezen

Projekti

• Financer: EC - European Commission
• Program financ.: H2020
• Številka projekta: 765581
• Naslov: Multidisciplinary European Joint Doctorate in the Design and Development of Glyco Drugs
• Akronim: PhD4GlycoDrug