dc.contributor.author | Zhu, Congrui | |
dc.contributor.author | El Qaidi, Samir | |
dc.contributor.author | McDonald, Peter | |
dc.contributor.author | Roy, Anuradha | |
dc.contributor.author | Hardwidge, Philip R. | |
dc.date.accessioned | 2022-01-07T20:46:09Z | |
dc.date.available | 2022-01-07T20:46:09Z | |
dc.date.issued | 2021-02-23 | |
dc.identifier.citation | Zhu, C.; El Qaidi, S.; McDonald, P.; Roy, A.; Hardwidge, P.R. YM155 Inhibits NleB and SseK Arginine Glycosyltransferase Activity. Pathogens 2021, 10, 253. https://doi.org/10.3390/pathogens10020253 | en_US |
dc.identifier.uri | http://hdl.handle.net/1808/32370 | |
dc.description.abstract | The type III secretion system effector proteins NleB and SseK are glycosyltransferases that glycosylate protein substrates on arginine residues. We conducted high-throughput screening assays on 42,498 compounds to identify NleB/SseK inhibitors. Such small molecules may be useful as mechanistic probes and may have utility in the eventual development of anti-virulence therapies against enteric bacterial pathogens. We observed that YM155 (sepantronium bromide) inhibits the activity of Escherichia coli NleB1, Citrobacter rodentium NleB, and both Salmonella enterica SseK1 and SseK2. YM155 was not toxic to mammalian cells, nor did it show cross-reactivity with the mammalian O-linked N-acetylglucosaminyltransferase (OGT). YM155 reduced Salmonella survival in mouse macrophage-like cells but had no direct impact on bacterial growth rates, suggesting YM155 may have utility as a potential anti-virulence inhibitor. | en_US |
dc.publisher | MDPI | en_US |
dc.rights | © 2021 by the authors. Licensee MDPI, Basel, Switzerland. This article is an open access article distributed under the terms and conditions of the Creative Commons Attribution (CC BY) license. | en_US |
dc.rights.uri | http://creativecommons.org/licenses/by/4.0/ | en_US |
dc.subject | Type three secretion system effectors | en_US |
dc.subject | Glycosyltransferase | en_US |
dc.subject | Enteric bacteria | en_US |
dc.title | YM155 Inhibits NleB and SseK Arginine Glycosyltransferase Activity | en_US |
dc.type | Article | en_US |
kusw.kuauthor | McDonald, Peter | |
kusw.kuauthor | Roy, Anuradha | |
kusw.kudepartment | High Throughput Screening Laboratory | en_US |
dc.identifier.doi | 10.3390/pathogens10020253 | en_US |
dc.identifier.orcid | https://orcid.org/ 0000-0002-0905-9979 | en_US |
kusw.oaversion | Scholarly/refereed, publisher version | en_US |
kusw.oapolicy | This item meets KU Open Access policy criteria. | en_US |
dc.identifier.pmid | PMC7926936 | en_US |
dc.rights.accessrights | openAccess | en_US |