8TO4
EGFR(T790M/V948R) in complex with the allosteric inhibitor FRF-06-057
Functional Information from PROSITE/UniProt
| site_id | PS00107 |
| Number of Residues | 28 |
| Details | PROTEIN_KINASE_ATP Protein kinases ATP-binding region signature. LGSGAFGTVYkGlwipegekvkip......VAIK |
| Chain | Residue | Details |
| D | LEU718-LYS745 |
| site_id | PS00109 |
| Number of Residues | 13 |
| Details | PROTEIN_KINASE_TYR Tyrosine protein kinases specific active-site signature. LVHrDLAARNVLV |
| Chain | Residue | Details |
| D | LEU833-VAL845 |
Functional Information from SwissProt/UniProt
| site_id | SWS_FT_FI1 |
| Number of Residues | 4 |
| Details | ACT_SITE: Proton acceptor => ECO:0000255|PROSITE-ProRule:PRU00159, ECO:0000255|PROSITE-ProRule:PRU10028 |
| Chain | Residue | Details |
| D | ASP837 | |
| A | ASP837 | |
| B | ASP837 | |
| C | ASP837 |
| site_id | SWS_FT_FI2 |
| Number of Residues | 4 |
| Details | BINDING: BINDING => ECO:0000269|PubMed:19563760, ECO:0007744|PDB:2GS7, ECO:0007744|PDB:3GT8, ECO:0007744|PDB:4ZSE, ECO:0007744|PDB:5CNN, ECO:0007744|PDB:5CNO, ECO:0007744|PDB:5D41 |
| Chain | Residue | Details |
| D | LEU718 | |
| A | LEU718 | |
| B | LEU718 | |
| C | LEU718 |
| site_id | SWS_FT_FI3 |
| Number of Residues | 4 |
| Details | BINDING: BINDING => ECO:0000269|PubMed:17349580, ECO:0000269|PubMed:19563760, ECO:0007744|PDB:2EB3, ECO:0007744|PDB:2GS7, ECO:0007744|PDB:2ITN, ECO:0007744|PDB:3GT8, ECO:0007744|PDB:3VJN, ECO:0007744|PDB:3VJO, ECO:0007744|PDB:4RIW, ECO:0007744|PDB:4RIY, ECO:0007744|PDB:4ZSE, ECO:0007744|PDB:5CNN, ECO:0007744|PDB:5CNO, ECO:0007744|PDB:5D41 |
| Chain | Residue | Details |
| D | LYS745 | |
| A | LYS745 | |
| B | LYS745 | |
| C | LYS745 |
| site_id | SWS_FT_FI4 |
| Number of Residues | 4 |
| Details | BINDING: BINDING => ECO:0000269|PubMed:17349580, ECO:0000269|PubMed:19563760, ECO:0007744|PDB:2EB3, ECO:0007744|PDB:2GS7, ECO:0007744|PDB:2ITN, ECO:0007744|PDB:2ITV, ECO:0007744|PDB:2ITX, ECO:0007744|PDB:3GT8, ECO:0007744|PDB:3VJN, ECO:0007744|PDB:3VJO, ECO:0007744|PDB:4RIW, ECO:0007744|PDB:4RIX, ECO:0007744|PDB:4RIY, ECO:0007744|PDB:4ZSE, ECO:0007744|PDB:5CNN, ECO:0007744|PDB:5CNO, ECO:0007744|PDB:5D41 |
| Chain | Residue | Details |
| D | MET790 | |
| A | MET790 | |
| B | MET790 | |
| C | MET790 |
| site_id | SWS_FT_FI5 |
| Number of Residues | 4 |
| Details | BINDING: BINDING => ECO:0000269|PubMed:17349580, ECO:0000269|PubMed:19563760, ECO:0007744|PDB:2EB3, ECO:0007744|PDB:2GS7, ECO:0007744|PDB:2ITN, ECO:0007744|PDB:2ITV, ECO:0007744|PDB:2ITX, ECO:0007744|PDB:3GT8, ECO:0007744|PDB:3VJN, ECO:0007744|PDB:4RIW, ECO:0007744|PDB:4RIX, ECO:0007744|PDB:4RIY, ECO:0007744|PDB:4ZSE, ECO:0007744|PDB:5CNN, ECO:0007744|PDB:5CNO, ECO:0007744|PDB:5D41 |
| Chain | Residue | Details |
| D | ASP855 | |
| A | ASP855 | |
| B | ASP855 | |
| C | ASP855 |
| site_id | SWS_FT_FI6 |
| Number of Residues | 4 |
| Details | SITE: Important for interaction with PIK3C2B |
| Chain | Residue | Details |
| D | TYR1016 | |
| A | TYR1016 | |
| B | TYR1016 | |
| C | TYR1016 |
| site_id | SWS_FT_FI7 |
| Number of Residues | 4 |
| Details | MOD_RES: Phosphoserine => ECO:0000269|PubMed:3138233, ECO:0007744|PubMed:18691976 |
| Chain | Residue | Details |
| D | SER695 | |
| A | SER695 | |
| B | SER695 | |
| C | SER695 |
| site_id | SWS_FT_FI8 |
| Number of Residues | 4 |
| Details | MOD_RES: N6-(2-hydroxyisobutyryl)lysine => ECO:0000269|PubMed:29192674 |
| Chain | Residue | Details |
| D | LYS745 | |
| A | LYS745 | |
| B | LYS745 | |
| C | LYS745 |
| site_id | SWS_FT_FI9 |
| Number of Residues | 4 |
| Details | MOD_RES: Phosphotyrosine => ECO:0000269|PubMed:23774213 |
| Chain | Residue | Details |
| D | TYR869 | |
| A | TYR869 | |
| B | TYR869 | |
| C | TYR869 |
| site_id | SWS_FT_FI10 |
| Number of Residues | 4 |
| Details | MOD_RES: Phosphoserine => ECO:0000269|PubMed:16083266, ECO:0007744|PubMed:18669648, ECO:0007744|PubMed:20068231, ECO:0007744|PubMed:24275569 |
| Chain | Residue | Details |
| D | SER991 | |
| A | SER991 | |
| B | SER991 | |
| C | SER991 |
| site_id | SWS_FT_FI11 |
| Number of Residues | 4 |
| Details | MOD_RES: Phosphoserine => ECO:0007744|PubMed:18669648 |
| Chain | Residue | Details |
| D | SER995 | |
| A | SER995 | |
| B | SER995 | |
| C | SER995 |
| site_id | SWS_FT_FI12 |
| Number of Residues | 4 |
| Details | MOD_RES: Phosphotyrosine; by autocatalysis => ECO:0000269|PubMed:19563760, ECO:0007744|PubMed:18669648 |
| Chain | Residue | Details |
| D | TYR998 | |
| A | TYR998 | |
| B | TYR998 | |
| C | TYR998 |
| site_id | SWS_FT_FI13 |
| Number of Residues | 4 |
| Details | MOD_RES: Phosphotyrosine; by autocatalysis => ECO:0000269|PubMed:19563760, ECO:0000269|PubMed:23774213 |
| Chain | Residue | Details |
| D | TYR1016 | |
| A | TYR1016 | |
| B | TYR1016 | |
| C | TYR1016 |
| site_id | SWS_FT_FI14 |
| Number of Residues | 16 |
| Details | CROSSLNK: Glycyl lysine isopeptide (Lys-Gly) (interchain with G-Cter in ubiquitin) => ECO:0000269|PubMed:16543144, ECO:0000269|PubMed:33996800 |
| Chain | Residue | Details |
| D | LYS716 | |
| B | LYS737 | |
| B | LYS754 | |
| B | LYS867 | |
| C | LYS716 | |
| C | LYS737 | |
| C | LYS754 | |
| C | LYS867 | |
| D | LYS737 | |
| D | LYS754 | |
| D | LYS867 | |
| A | LYS716 | |
| A | LYS737 | |
| A | LYS754 | |
| A | LYS867 | |
| B | LYS716 |
| site_id | SWS_FT_FI15 |
| Number of Residues | 12 |
| Details | CROSSLNK: Glycyl lysine isopeptide (Lys-Gly) (interchain with G-Cter in ubiquitin) => ECO:0000269|PubMed:16543144 |
| Chain | Residue | Details |
| C | LYS929 | |
| C | LYS970 | |
| D | LYS929 | |
| D | LYS970 | |
| A | LYS929 | |
| A | LYS970 | |
| B | LYS929 | |
| B | LYS970 |
| site_id | SWS_FT_FI16 |
| Number of Residues | 8 |
| Details | CROSSLNK: Glycyl lysine isopeptide (Lys-Gly) (interchain with G-Cter in ubiquitin) => ECO:0000269|PubMed:33996800 |
| Chain | Residue | Details |
| D | LYS757 | |
| D | LYS960 | |
| A | LYS757 | |
| A | LYS960 | |
| B | LYS757 | |
| B | LYS960 | |
| C | LYS757 | |
| C | LYS960 |
