XSB0592 : Chain A, Egfr Kinase Domain Complexed With A Quinazoline Inhibitor- Gw572016
[ CaMP Format ]
This entry is computationally expanded from SB0050
* Basic Information
| Organism | Homo sapiens (human) |
| Protein Names | Epidermal growth factor receptor; 2.7.10.1; Receptor tyrosine-protein kinase ErbB-1 |
| Gene Names | ERBB1 |
| Gene Locus | Not available |
| GO Function | Not available |
* Information From OMIM
Not Available.
* Structure Information
1. Primary Information
Length: 352 aa
Average Mass: 40.269 kDa
Monoisotopic Mass: 40.243 kDa
2. Domain Information
Annotated Domains: interpro / pfam / smart / prosite
Computationally Assigned Domains (Pfam+HMMER):
| domain name | begin | end | score | e-value |
|---|---|---|---|---|
| --- cleavage 13 --- | ||||
| Pkinase_Tyr 1. | 42 | 298 | 439.6 | 4.7e-129 |
3. Sequence Information
Fasta Sequence: XSB0592.fasta
Amino Acid Sequence and Secondary Structures (PsiPred):
4. 3D Information
Known Structures in PDB: 1DNQ (Model; -; A=25-336), 1DNR (Model; -; A=337-645), 1IVO (X-ray; 330 A; A/B=25-646), 1M14 (X-ray; 260 A; A=695-1022), 1M17 (X-ray; 260 A; A=695-1022), 1MOX (X-ray; 250 A; A/B=25-525), 1NQL (X-ray; 280 A; A=25-642), 1XKK (X-ray; 240 A; A=695-1022), 1YY9 (X-ray; 260 A; A=25-642), 1Z9I (NMR; -; A=669-721), 2EB2 (X-ray; 250 A; A=695-1022), 2EB3 (X-ray; 284 A; A=695-1022), 2EXP (Model; -; A=311-326), 2EXQ (Model; -; A=27-536), 2GS2 (X-ray; 280 A; A=696-1022), 2GS6 (X-ray; 260 A; A=696-1022), 2GS7 (X-ray; 260 A; A/B=696-1022), 2ITN (X-ray; 247 A; A=696-1019), 2ITO (X-ray; 325 A; A=696-1022), 2ITP (X-ray; 274 A; A=696-1022), 2ITQ (X-ray; 268 A; A=696-1022), 2ITT (X-ray; 273 A; A=696-1022), 2ITU (X-ray; 280 A; A=696-1022), 2ITV (X-ray; 247 A; A=696-1022), 2ITW (X-ray; 288 A; A=696-1022), 2ITX (X-ray; 298 A; A=696-1022), 2ITY (X-ray; 342 A; A=696-1022), 2ITZ (X-ray; 272 A; A=696-1022), 2J5E (X-ray; 310 A; A=696-1022), 2J5F (X-ray; 300 A; A=696-1022), 2J6M (X-ray; 310 A; A=696-1022), 2JIT (X-ray; 310 A; A/B=696-1022), 2JIU (X-ray; 305 A; A/B=695-1022), 2JIV (X-ray; 350 A; A/B=695-1022), 2RF9 (X-ray; 350 A; A/B=696-1022), 2RFD (X-ray; 360 A; A/B=702-1022), 2RFE (X-ray; 290 A; A/B/C/D=702-1022), 2RGP (X-ray; 200 A; A=702-1016), 3B2U (X-ray; 258 A; A/B/E/I/M/P/S/V=335-538), 3B2V (X-ray; 330 A; A=25-642), 3BEL (X-ray; 230 A; A=702-1016), 3BUO (X-ray; 260 A; A/C=1063-1075), 3C09 (X-ray; 320 A; A/D=335-538)
* Cleavage Information
1 [sites]
Cleavage sites (±10aa)
[Site 1] GHHHHHHDYD13-IPTTENLYFQ
Asp13 
Ile
 |
|||||||||
| P10 | P9 | P8 | P7 | P6 | P5 | P4 | P3 | P2 | P1 |
|---|---|---|---|---|---|---|---|---|---|
| Gly4 | His5 | His6 | His7 | His8 | His9 | His10 | Asp11 | Tyr12 | Asp13 |
 |
|||||||||
| P1' | P2' | P3' | P4' | P5' | P6' | P7' | P8' | P9' | P10' |
| Ile14 | Pro15 | Thr16 | Thr17 | Glu18 | Asn19 | Leu20 | Tyr21 | Phe22 | Gln23 |
Sequence conservation (by blast)
* References
[PubMed ID: 15374980] Wood ER, Truesdale AT, McDonald OB, Yuan D, Hassell A, Dickerson SH, Ellis B, Pennisi C, Horne E, Lackey K, Alligood KJ, Rusnak DW, Gilmer TM, Shewchuk L, A unique structure for epidermal growth factor receptor bound to GW572016 (Lapatinib): relationships among protein conformation, inhibitor off-rate, and receptor activity in tumor cells. Cancer Res. 2004 Sep 15;64(18):6652-9.