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dc.contributor.authorChu, Jenniferen_US
dc.contributor.authorZhang, Wenhanen_US
dc.contributor.authorCencic, Reginaen_US
dc.contributor.authorDevine, William G.en_US
dc.contributor.authorBeglov, Dmitrien_US
dc.contributor.authorHenkel, Thomasen_US
dc.contributor.authorBrown, Lauren E.en_US
dc.contributor.authorVajda, Sandoren_US
dc.contributor.authorPorco, John A.en_US
dc.contributor.authorPelletier, Jerryen_US
dc.coverage.spatialUnited Statesen_US
dc.date2019-08-21
dc.date.accessioned2020-12-15T16:27:56Z
dc.date.available2020-12-15T16:27:56Z
dc.date.issued2019-11-21
dc.identifierhttps://www.ncbi.nlm.nih.gov/pubmed/31519508
dc.identifier.citationJennifer Chu, Wenhan Zhang, Regina Cencic, William G Devine, Dmitri Beglov, Thomas Henkel, Lauren E Brown, Sandor Vajda, John A Porco, Jerry Pelletier. 2019. "Amidino-Rocaglates: A Potent Class of eIF4A Inhibitors.." Cell Chem Biol, Volume 26, Issue 11, pp. 1586 - 1593.e3. https://doi.org/10.1016/j.chembiol.2019.08.008
dc.identifier.issn2451-9448
dc.identifier.urihttps://hdl.handle.net/2144/41805
dc.descriptionPublished in final edited form as: Cell Chem Biol. 2019 November 21; 26(11): 1586–1593.e3. doi:10.1016/j.chembiol.2019.08.008.en_US
dc.description.abstractRocaglates share a common cyclopenta[b]benzofuran core that inhibits eukaryotic translation initiation by modifying the behavior of the RNA helicase, eIF4A. Working as interfacial inhibitors, rocaglates stabilize the association between eIF4A and RNA, which can lead to the formation of steric barriers that block initiating ribosomes. There is significant interest in the development and expansion of rocaglate derivatives, as several members of this family have been shown to possess potent anti-neoplastic activity in vitro and in vivo. To further our understanding of rocaglate diversity and drug design, herein we explore the RNA clamping activity of >200 unique rocaglate derivatives. Through this, we report on the identification and characterization of a potent class of synthetic rocaglates called amidino-rocaglates. These compounds are among the most potent rocaglates documented to date and, taken together, this work offers important information that will guide the future design of rocaglates with improved biological properties.en_US
dc.description.sponsorshipP50 GM067041 - NIGMS NIH HHS; R24 GM111625 - NIGMS NIH HHS; R35 GM118078 - NIGMS NIH HHS; R35 GM118173 - NIGMS NIH HHS; Canadian Institutes of Health Research Foundationen_US
dc.format.extentp. 1586 - 1593.e3en_US
dc.languageeng
dc.language.isoen_US
dc.relation.ispartofCell Chem Biol
dc.subjectAmidino-rocaglatesen_US
dc.subjecteIF4Aen_US
dc.subjecteIF4Fen_US
dc.subjectInterfacial inhibitoren_US
dc.subjectTranslation initiationen_US
dc.subjectAmidinesen_US
dc.subjectAnimalsen_US
dc.subjectAntineoplastic agentsen_US
dc.subjectBenzofuransen_US
dc.subjectCell survivalen_US
dc.subjectDEAD-box RNA helicasesen_US
dc.subjectDrug designen_US
dc.subjectEukaryotic initiation factor-4Aen_US
dc.subjectFemaleen_US
dc.subjectHumansen_US
dc.subjectLymphomaen_US
dc.subjectMiceen_US
dc.subjectMice, inbred C57BLen_US
dc.subjectProtein biosynthesisen_US
dc.subjectRNAen_US
dc.subjectRecombinant proteinsen_US
dc.subjectRibosomesen_US
dc.subjectStructure-activity relationshipen_US
dc.titleAmidino-rocaglates: a potent class of eIF4A inhibitorsen_US
dc.typeArticleen_US
dc.description.versionAccepted manuscripten_US
dc.identifier.doi10.1016/j.chembiol.2019.08.008
pubs.elements-sourcepubmeden_US
pubs.notesEmbargo: Not knownen_US
pubs.organisational-groupBoston Universityen_US
pubs.organisational-groupBoston University, College of Arts & Sciencesen_US
pubs.organisational-groupBoston University, College of Arts & Sciences, Department of Chemistryen_US
pubs.organisational-groupBoston University, College of Engineeringen_US
pubs.publication-statusPublisheden_US
dc.identifier.mycv488421


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