ArticleJournal of the American Chemical Society2026
Benzoxaboroles Are Structurally Unique Binders of Eukaryotic Translation Initiation Factor 4E.
Joshua B Combs, D Matthew Peacock, Gregory B Craven, Sungwon Jung, Ying Chen, Sang M Le, Jack Taunton, Kevan M Shokat
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In one paragraphArticle in Journal of the American Chemical Society, 2026. The graph could read no effect estimate from its abstract, so it casts no vote on the map. Not yet cited in PubMed.
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2 · The registryThe trial behind it
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4 · The recordCorrections and comments
5 · Who and what moneyAuthors and funding
8 authors.
Joshua B CombsDepartment of Cellular and Molecular Pharmacology, University of California San Francisco, San Francisco, California 94158, United States.
D Matthew PeacockDepartment of Cellular and Molecular Pharmacology, University of California San Francisco, San Francisco, California 94158, United States.
Gregory B CravenDepartment of Cellular and Molecular Pharmacology, University of California San Francisco, San Francisco, California 94158, United States.
Sungwon JungDepartment of Cellular and Molecular Pharmacology, University of California San Francisco, San Francisco, California 94158, United States.
Ying ChenDepartment of Cellular and Molecular Pharmacology, University of California San Francisco, San Francisco, California 94158, United States.
Sang M LeDepartment of Cellular and Molecular Pharmacology, University of California San Francisco, San Francisco, California 94158, United States.
Jack TauntonDepartment of Cellular and Molecular Pharmacology, University of California San Francisco, San Francisco, California 94158, United States.ORCID 0000-0002-9627-5898 Kevan M ShokatDepartment of Cellular and Molecular Pharmacology, University of California San Francisco, San Francisco, California 94158, United States.ORCID 0000-0001-8590-7741 Funding
Molecular and Cellular Mechanisms in CancerT32CA108462 · NCI · UNIVERSITY OF CALIFORNIA, SAN FRANCISCO · PI GOGA, ANDREI · 2004 to 2024
$10.4MMechanisms and models of C11or95 and C11or95-RELA fusions (RELAFus )U54CA243125 · NCI · FRED HUTCHINSON CANCER RESEARCH CENTER · PI HOLLAND, ERIC C. · 2019 to 2022
$6.2MInhibitors of the G protein GNAS which drives pancreatic tumorigenesisR01CA244550 · NCI · UNIVERSITY OF CALIFORNIA, SAN FRANCISCO · PI SHOKAT, KEVAN M. · 2020 to 2024
$2.0MTargeting the GTP-bound state of oncogenic Ras proteinsF32CA253966 · NCI · UNIVERSITY OF CALIFORNIA, SAN FRANCISCO · PI PEACOCK, DAVID MATTHEW · 2020 to 2021
$134kNCI NIH HHS F32 CA253966NCI NIH HHS R01 CA244550NCI NIH HHS T32 CA108462NCI NIH HHS U54 CA243125
6 · The paper itselfAbstract
Benzoxaboroles offer unusual reactivity and protein recognition for the development of small molecule drugs. Despite this potential, they are uncommon in drug discovery or in fragment screening libraries. We synthesized a series of structurally related benzoxaboroles containing a diazirine/alkyne tag to enable in-cell photoaffinity labeling experiments. A subset of this library was found to have high selectivity for eukaryotic translation initiation factor 4E (eIF4E). The benzoxaborole-eIF4E interaction was found to be stereoselective in nature and competitive with the 7-methylguanosine cap of mRNA. Site of labeling experiments revealed that the benzoxaborole fragment interacts with the cap binding pocket of eIF4E.
Indexed as
Boron CompoundsEukaryotic Initiation Factor-4EBinding SitesModels, MolecularMolecular StructureProtein BindingBoron CompoundsEukaryotic Initiation Factor-4E
Identifiers
PMID42424620
PMCPMC13397561
What Socratic holds
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LicenceCC BY
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