2018
Editing N-Glycan Site Occupancy with Small-Molecule Oligosaccharyltransferase Inhibitors
Rinis N, Golden JE, Marceau CD, Carette JE, Van Zandt MC, Gilmore R, Contessa JN. Editing N-Glycan Site Occupancy with Small-Molecule Oligosaccharyltransferase Inhibitors. Cell Chemical Biology 2018, 25: 1231-1241.e4. PMID: 30078634, PMCID: PMC6337728, DOI: 10.1016/j.chembiol.2018.07.005.Peer-Reviewed Original ResearchMeSH KeywordsBenzamidesCatalytic DomainDrug Evaluation, PreclinicalEnzyme InhibitorsGene Knockout TechniquesHEK293 CellsHexosyltransferasesHumansMembrane ProteinsStructure-Activity RelationshipSulfonamidesConceptsNGI-1Cellular unfolded protein responseMultisubunit enzyme complexN-glycan site occupancyUnfolded protein responseSubset of glycoproteinsSubunit-specific inhibitorsSecretory pathwayCatalytic subunitProtein responseEnzyme complexTarget proteinsOligosaccharyltransferasePharmacologic inhibitionGlycosylationProteinCell modelBiological effectsInhibitorsStructure-activity relationshipsSTT3BSTT3APharmacological approachesSubunitsSite occupancy
2016
Oligosaccharyltransferase inhibition induces senescence in RTK-driven tumor cells
Lopez-Sambrooks C, Shrimal S, Khodier C, Flaherty DP, Rinis N, Charest JC, Gao N, Zhao P, Wells L, Lewis TA, Lehrman MA, Gilmore R, Golden JE, Contessa JN. Oligosaccharyltransferase inhibition induces senescence in RTK-driven tumor cells. Nature Chemical Biology 2016, 12: 1023-1030. PMID: 27694802, PMCID: PMC5393272, DOI: 10.1038/nchembio.2194.Peer-Reviewed Original ResearchMeSH KeywordsBenzamidesCell Cycle CheckpointsCell Line, TumorCell ProliferationCellular SenescenceDose-Response Relationship, DrugEnzyme InhibitorsHexosyltransferasesHigh-Throughput Screening AssaysHumansMembrane ProteinsMolecular StructureReceptor Protein-Tyrosine KinasesStructure-Activity RelationshipSulfonamides