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A noncanonical function of EIF4E limits ALDH1B1 activity and increases susceptibility to ferroptosis.
Chen X, Huang J, Yu C, Liu J, Gao W, Li J, Song X, Zhou Z, Li C, Xie Y, Kroemer G, Liu J, Tang D, Kang R. Chen X, et al. Nat Commun. 2022 Oct 23;13(1):6318. doi: 10.1038/s41467-022-34096-w. Nat Commun. 2022. PMID: 36274088 Free PMC article.
Here, we report an unexpected role for the eukaryotic translation initiation factor EIF4E as a determinant of ferroptotic sensitivity by controlling lipid peroxidation. A drug screening identified 4EGI-1 and 4E1RCat (previously known as EIF4E-EIF4G1 interaction inhibitors) …
Here, we report an unexpected role for the eukaryotic translation initiation factor EIF4E as a determinant of ferroptotic sensitivity by con …
In Silico Drug Repurposing by Structural Alteration after Induced Fit: Discovery of a Candidate Agent for Recovery of Nucleotide Excision Repair in Xeroderma Pigmentosum Group D Mutant (R683W).
Takaoka Y, Ohta M, Tateishi S, Sugano A, Nakano E, Miura K, Suzuki T, Nishigori C. Takaoka Y, et al. Biomedicines. 2021 Mar 3;9(3):249. doi: 10.3390/biomedicines9030249. Biomedicines. 2021. PMID: 33802476 Free PMC article.
UDS values of the cells improved about 1.4-1.7 times after 4E1RCat treatment compared with solvent-only controls; aprepitant showed no positive effect. In this study, therefore, we succeeded in finding the candidate agent 4E1RCat for XPD R683W. We also demonstrated …
UDS values of the cells improved about 1.4-1.7 times after 4E1RCat treatment compared with solvent-only controls; aprepitant showed n …
eIF4E-eIF4G complex inhibition synergistically enhances the effect of sorafenib in hepatocellular carcinoma.
Fang C, Xie H, Zhao J, Wang W, Hou H, Zhang B, Zhou D, Geng X. Fang C, et al. Anticancer Drugs. 2021 Sep 1;32(8):822-828. doi: 10.1097/CAD.0000000000001074. Anticancer Drugs. 2021. PMID: 33783376 Free PMC article.
The specific mechanism was demonstrated using western blot and lentivirus transfection. The combination of sorafenib with eIF4E-eIF4G inhibitors 4E1RCat (structural) or 4EGI-1 (competitive) synergistically inhibited the cell viability and colony formation ability of HCC ce …
The specific mechanism was demonstrated using western blot and lentivirus transfection. The combination of sorafenib with eIF4E-eIF4G inhibi …
Targeting SARS-CoV-2 nucleocapsid oligomerization: Insights from molecular docking and molecular dynamics simulations.
Ahamad S, Gupta D, Kumar V. Ahamad S, et al. J Biomol Struct Dyn. 2022 Apr;40(6):2430-2443. doi: 10.1080/07391102.2020.1839563. Epub 2020 Nov 3. J Biomol Struct Dyn. 2022. PMID: 33140703 Free PMC article.
Herein, multiple computational approaches were employed to explore the potential mechanisms of binding and inhibitor activity of five antiviral drugs toward CTD. The five anti-N drugs studied in this work are 4E1RCat, Silmitasertib, TMCB, Sapanisertib, and Rapamycin. Among …
Herein, multiple computational approaches were employed to explore the potential mechanisms of binding and inhibitor activity of five antivi …
Salubrinal in Combination With 4E1RCat Synergistically Impairs Melanoma Development by Disrupting the Protein Synthetic Machinery.
Kardos GR, Gowda R, Dinavahi SS, Kimball S, Robertson GP. Kardos GR, et al. Front Oncol. 2020 Jun 19;10:834. doi: 10.3389/fonc.2020.00834. eCollection 2020. Front Oncol. 2020. PMID: 32637352 Free PMC article.
While salubrinal alone was ineffective, the combined use of salubrinal and 4E1RCat (a dual inhibitor of eIF4E:4E-BP1 and eIF4E:eIF4G interaction to prevent assembly of the eIF4F complex and inhibit cap-dependent translation) was found to be effective at decreasing protein …
While salubrinal alone was ineffective, the combined use of salubrinal and 4E1RCat (a dual inhibitor of eIF4E:4E-BP1 and eIF4E:eIF4G …
Crimean-Congo Hemorrhagic Fever Virus Nucleocapsid Protein Augments mRNA Translation.
Jeeva S, Cheng E, Ganaie SS, Mir MA. Jeeva S, et al. J Virol. 2017 Jul 12;91(15):e00636-17. doi: 10.1128/JVI.00636-17. Print 2017 Aug 1. J Virol. 2017. PMID: 28515298 Free PMC article.
Unlike the canonical host translation machinery, inhibition of eIF4F complex, an amalgam of three initiation factors, eIF4A, eIF4G, and eIF4E, by the chemical inhibitor 4E1RCat did not impact the CCHFV-NP-mediated translation mechanism. ...
Unlike the canonical host translation machinery, inhibition of eIF4F complex, an amalgam of three initiation factors, eIF4A, eIF4G, and eIF4 …
CDK1 substitutes for mTOR kinase to activate mitotic cap-dependent protein translation.
Shuda M, Velásquez C, Cheng E, Cordek DG, Kwun HJ, Chang Y, Moore PS. Shuda M, et al. Proc Natl Acad Sci U S A. 2015 May 12;112(19):5875-82. doi: 10.1073/pnas.1505787112. Epub 2015 Apr 16. Proc Natl Acad Sci U S A. 2015. PMID: 25883264 Free PMC article.
Using a Click-iT flow cytometric assay to directly measure mitotic protein synthesis, we find that most new protein synthesis during mitosis is cap-dependent, a result confirmed using the eIF4E/4G inhibitor drug 4E1RCat. For most cell lines tested, cap-dependent translatio …
Using a Click-iT flow cytometric assay to directly measure mitotic protein synthesis, we find that most new protein synthesis during mitosis …
Regulation of cardiac expression of the diabetic marker microRNA miR-29.
Arnold N, Koppula PR, Gul R, Luck C, Pulakat L. Arnold N, et al. PLoS One. 2014 Jul 25;9(7):e103284. doi: 10.1371/journal.pone.0103284. eCollection 2014. PLoS One. 2014. PMID: 25062042 Free PMC article.
Moreover, inhibition of either mTORC1 substrate S6K1 by PF-4708671, or eIF4E-induced translation by 4E1RCat suppressed MCL-1. We used Zucker diabetic fatty (ZDF) rat, a rodent model for DM, to test whether dysregulation of cardiac miR-29-MCL-1 axis correlates with DM progr …
Moreover, inhibition of either mTORC1 substrate S6K1 by PF-4708671, or eIF4E-induced translation by 4E1RCat suppressed MCL-1. We used …