5SX4
Crystal Structure of panitumumab in complex with epidermal growth factor receptor domain 3.
Summary for 5SX4
| Entry DOI | 10.2210/pdb5sx4/pdb |
| Related | 5SX5 |
| Descriptor | Panitumumab Fab Light Chain, Panitumumab Fab Heavy Chain, Epidermal growth factor receptor, ... (8 entities in total) |
| Functional Keywords | cetuximab, panitumumab, egfr, vectibix, erbitux, transferase-immune system complex, transferase/immune system |
| Biological source | Homo sapiens More |
| Cellular location | Cell membrane; Single-pass type I membrane protein. Isoform 2: Secreted: P00533 |
| Total number of polymer chains | 6 |
| Total formula weight | 140068.46 |
| Authors | Sickmier, E.A.,Kurzeja, R.J.M.,Michelsen, K.,Mukta, V.,Yang, E.,Tasker, A.S. (deposition date: 2016-08-09, release date: 2016-10-05, Last modification date: 2024-10-16) |
| Primary citation | Sickmier, E.A.,Kurzeja, R.J.,Michelsen, K.,Vazir, M.,Yang, E.,Tasker, A.S. The Panitumumab EGFR Complex Reveals a Binding Mechanism That Overcomes Cetuximab Induced Resistance. Plos One, 11:e0163366-e0163366, 2016 Cited by PubMed Abstract: Panitumumab and cetuximab target the epidermal growth factor receptor for the treatment of metastatic colorectal cancer. These therapies provide a significant survival benefit to patients with metastatic colorectal cancer with wild-type RAS. A single point mutation in the ectodomain of EGFR (S468R) confers acquired or secondary resistance in cetuximab treated patients, which is not observed in panitumumab-treated patients. Structural and biophysical studies presented here show this mutation directly blocks cetuximab binding to EGFR domain III and describes a unique mechanism by which panitumumab uses a central cavity to accommodate this mutation. PubMed: 27658254DOI: 10.1371/journal.pone.0163366 PDB entries with the same primary citation |
| Experimental method | X-RAY DIFFRACTION (2.8 Å) |
Structure validation
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