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Inhibition of O-GlcNAc transferase (OGT) by peptidic hybridsZhao, Han, pharmacist ...O-GlcNAc transferase (OGT) attaches a GlcNAc moiety on specific substrate proteins using UDP-GlcNAc as the sugar donor. This modification can alter protein function by regulating cellular signaling ... and transcription pathways in response to altered nutrient availability and stress. Specific inhibitors of OGT would be valuable tools for biological studies and lead structures for therapeutics. The existing OGT inhibitors are mainly derived from the sugar donor substrate, but poor cell permeability and off-target effects limit their use. Here, we describe our progress on OGT inhibition based on substrate peptides identified by array screening. Subsequently, bisubstrate inhibitors were prepared by conjugating these peptides to uridine in various ways. In parallel, an in silico fragment screening was conducted to obtain small molecules targeting the UDP binding pocket. After evaluation of the initial hits, one of these small molecules was elaborated into a novel OGT hybrid inhibitor, as the replacement of uridine. The novel compounds inhibit OGT activity with IC50 values in the micromolar range.Source: MedChemComm. - ISSN 2040-2503 (Vol. 9, iss. 5, 2018, str. 883-887)Type of material - article, component partPublish date - 2018Language - englishCOBISS.SI-ID - 4494449
Author
Zhao, Han, pharmacist |
Tomašič, Tihomir |
Shi, Jie |
Weiss, Matjaž |
Ruijtenbeek, Rob |
Anderluh, Marko |
Pieters, Roland J.
Topics
O-GlcNAc transferase |
peptidic hybrids |
biological studies |
stress
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Author | Zhao, Han, pharmacist ... |
Title | Inhibition of O-GlcNAc transferase (OGT) by peptidic hybrids |
Publication date | 2018-04-18 |
COBISS.SI-ID | 4494449 |
Publication version in repository | Publisher's version |
Publication licence | Creative Commons Attribution 4.0 International |
Embargo | Immediate publication for public |
Project(s) from which the publication was funded
Title | Acronym | Project ID | Funder |
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Farmacevtska kemija: načrtovanje, sinteza in vrednotenje učinkovin | P1-0208-2015 |
Javna agencija za znanstvenoraziskovalno in inovacijsko dejavnost Republike Slovenije |
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Database name | Field | Year |
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Links to authors' personal bibliographies | Links to information on researchers in the SICRIS system |
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Zhao, Han, pharmacist | ![]() |
Tomašič, Tihomir | 28334 |
Shi, Jie | ![]() |
Weiss, Matjaž | 50503 |
Ruijtenbeek, Rob | ![]() |
Anderluh, Marko | 21456 |
Pieters, Roland J. | ![]() |
Source: Personal bibliographies
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