7ZTL
Crystal structure of a covalently linked Aurora-A N-Myc complex
Summary for 7ZTL
| Entry DOI | 10.2210/pdb7ztl/pdb |
| Descriptor | Aurora kinase A, N-myc proto-oncogene protein, ADENOSINE-5'-DIPHOSPHATE, ... (9 entities in total) |
| Functional Keywords | crosslink, protein-protein-complex, transferase |
| Biological source | Homo sapiens (human) More |
| Total number of polymer chains | 2 |
| Total formula weight | 44177.12 |
| Authors | Diebold, M.,Schindelin, H. (deposition date: 2022-05-11, release date: 2023-01-18, Last modification date: 2024-11-06) |
| Primary citation | Diebold, M.,Schonemann, L.,Eilers, M.,Sotriffer, C.,Schindelin, H. Crystal structure of a covalently linked Aurora-A-MYCN complex. Acta Crystallogr D Struct Biol, 79:1-9, 2023 Cited by PubMed Abstract: Formation of the Aurora-A-MYCN complex increases levels of the oncogenic transcription factor MYCN in neuroblastoma cells by abrogating its degradation through the ubiquitin proteasome system. While some small-molecule inhibitors of Aurora-A were shown to destabilize MYCN, clinical trials have not been satisfactory to date. MYCN itself is considered to be `undruggable' due to its large intrinsically disordered regions. Targeting the Aurora-A-MYCN complex rather than Aurora-A or MYCN alone will open new possibilities for drug development and screening campaigns. To overcome the challenges that a ternary system composed of Aurora-A, MYCN and a small molecule entails, a covalently cross-linked construct of the Aurora-A-MYCN complex was designed, expressed and characterized, thus enabling screening and design campaigns to identify selective binders. PubMed: 36601802DOI: 10.1107/S2059798322011433 PDB entries with the same primary citation |
| Experimental method | X-RAY DIFFRACTION (1.9 Å) |
Structure validation
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