Table 1. Published crystal structures of EGFR-TK.
The table documents the EGFR-TK crystal structures currently published, including two recent EGFR-TK crystal structures in complex with anilinoquinazoline-based irreversible inhibitors 13-JAB and 34-JAB74.
| Protein Data Bank accession code |
Mutation | Inhibitor | Conformational State |
Space Group |
Resolution limit (Å2) |
Publication |
|---|---|---|---|---|---|---|
| 1M14 | Wild-Type | --- | active | I23 | 2.6 | Stamos (2002) |
| 1M17 | Wild-Type | erlotinib (Tarceva) | active | I23 | 2.6 | Stamos (2002) |
| 1XKK | Wild-Type | lapatinib (Tykerb) | inactive | P212121 | 2.4 | Wood (2004) |
| 2GS6 | Wild-Type | ATP analogue-peptide conjugate | active | I23 | 2.6 | Zhang (2006) |
| 2GS2 | Wild-Type | --- | active | I23 | 2.8 | Zhang (2006) |
| 2GS7 | V924R | AMP-PNP | inactive | P21 | 2.6 | Zhang (2006) |
| 2ITX | Wild-Type | AMP-PNP | active | I23 | 3.0 | Yun (2007) |
| 2J6M | Wild-Type | gefitinib (Iressa) | active | I23 | 3.1 | Yun (2007) |
| 2ITW | Wild-Type | AFN-941 | active | I23 | 2.9 | Yun (2007) |
| 2ITY | Wild-Type | gefitinib (Iressa) | active | I23 | 3.4 | Yun (2007) |
| 2ITN | G719S | AMP-PNP | active | I23 | 2.4 | Yun (2007) |
| 2ITO | G719S | gefitinib (Iressa) | active | I23 | 3.2 | Yun (2007) |
| 2ITP | G719S | AEE788 | active | I23 | 2.7 | Yun (2007) |
| 2ITQ | G719S | AFN-941 | active | I23 | 2.7 | Yun (2007) |
| 2ITT | L858R | AEE-788 | active | I23 | 2.7 | Yun (2007) |
| 2ITU | L858R | AFN-941 | active | I23 | 2.8 | Yun (2007) |
| 2ITV | L858R | AMP-PNP | active | I23 | 2.4 | Yun (2007) |
| 2ITZ | L858R | gefitinib (Iressa) | active | I23 | 2.8 | Yun (2007) |
| 2J5E | Wild-Type | 13-JAB | active | I23 | 3.1 | Blair (2007) |
| 2J5F | Wild-Type | 34-JAB | active | I23 | 2.95 | Blair (2007) |