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| 001 | 1010687 | ||
| 005 | 20240625095129.0 | ||
| 024 | 7 | _ | |a 10.3390/ijms241713127 |2 doi |
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| 100 | 1 | _ | |a Joseph, Benjamin Philipp |0 P:(DE-Juel1)179040 |b 0 |u fzj |
| 245 | _ | _ | |a Low Molecular Weight Inhibitors Targeting the RNA-Binding Protein HuR |
| 260 | _ | _ | |a Basel |c 2023 |b Molecular Diversity Preservation International |
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| 520 | _ | _ | |a The RNA-binding protein human antigen R (HuR) regulates stability, translation, and nucleus-to-cytoplasm shuttling of its target mRNAs. This protein has been progressively recognized as a relevant therapeutic target for several pathologies, like cancer, neurodegeneration, as well as inflammation. Inhibitors of mRNA binding to HuR might thus be beneficial against a variety of diseases. Here, we present the rational identification of structurally novel HuR inhibitors. In particular, by combining chemoinformatic approaches, high-throughput virtual screening, and RNA–protein pulldown assays, we demonstrate that the 4-(2-(2,4,6-trioxotetrahydropyrimidin-5(2H)-ylidene)hydrazineyl)benzoate ligand exhibits a dose-dependent HuR inhibition effect in binding experiments. Importantly, the chemical scaffold is new with respect to the currently known HuR inhibitors, opening up a new avenue for the design of pharmaceutical agents targeting this important protein. |
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| 700 | 1 | _ | |a Alfonso-Prieto, Mercedes |0 P:(DE-Juel1)169976 |b 4 |
| 700 | 1 | _ | |a Krauß, Sybille |0 P:(DE-HGF)0 |b 5 |e Corresponding author |
| 700 | 1 | _ | |a Carloni, Paolo |0 P:(DE-Juel1)145614 |b 6 |e Corresponding author |
| 700 | 1 | _ | |a Rossetti, Giulia |0 P:(DE-Juel1)145921 |b 7 |
| 773 | _ | _ | |a 10.3390/ijms241713127 |g Vol. 24, no. 17, p. 13127 - |0 PERI:(DE-600)2019364-6 |n 17 |p 13127 - |t International journal of molecular sciences |v 24 |y 2023 |x 1422-0067 |
| 856 | 4 | _ | |u https://juser.fz-juelich.de/record/1010687/files/ijms-24-13127-v3.pdf |y OpenAccess |
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