9DON
Crystal structure of eIF4e in complex with Compound 5-PA
This is a non-PDB format compatible entry.
Summary for 9DON
| Entry DOI | 10.2210/pdb9don/pdb |
| Descriptor | Eukaryotic translation initiation factor 4E, 7N-METHYL-8-HYDROGUANOSINE-5'-DIPHOSPHATE, 2-[3-[[2-azanyl-7-[(5-chloranyl-1-benzofuran-2-yl)methyl]-6-oxidanylidene-1~{H}-purin-9-yl]methyl]phenyl]ethylphosphonic acid, ... (4 entities in total) |
| Functional Keywords | eif4e, translation initiation inhibitor, translation |
| Biological source | Homo sapiens (human) |
| Total number of polymer chains | 2 |
| Total formula weight | 45553.78 |
| Authors | |
| Primary citation | Cardenas, E.L.,O'Rourke, R.L.,Menon, A.,Vega-Hernandez, G.,Meagher, J.,Stuckey, J.,Garner, A.L. Second-Generation Cap Analogue Prodrugs for Targeting Aberrant Eukaryotic Translation Initiation Factor 4E Activity in Cancer. Acs Med.Chem.Lett., 16:96-100, 2025 Cited by PubMed Abstract: Dysregulation of translation is a hallmark of cancer that enables rapid changes in cellular protein production to shape oncogenic phenotypes. Translation initiation is governed by the mGpppX cap-binding protein eukaryotic translation initiation factor 4E (eIF4E), the rate-limiting factor of cap-dependent translation initiation. eIF4E is overexpressed in many cancers and drives the production of oncoproteins that promote tumor growth and survival. Accordingly, eIF4E has been established as an attractive albeit challenging therapeutic target. Building upon our previous work of developing cell-permeable cap analogue prodrugs that inhibit eIF4E binding to the mGpppX cap, herein we disclose the design of second-generation cap analogues with alternative -9-substituted linkers which exhibit anticancer activity in BRAF mutant melanoma cell lines. PubMed: 39811141DOI: 10.1021/acsmedchemlett.4c00466 PDB entries with the same primary citation |
| Experimental method | X-RAY DIFFRACTION (2.091 Å) |
Structure validation
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