epidermal growth factor receptor

Nomenclature: epidermal growth factor receptor

Abbreviated Name: EGFR

Family: Receptor tyrosine kinases

Annotation status:  image of an orange circle Annotated and awaiting review. Please contact us if you can help with reviewing.  » Email us

Gene and Protein Information
Species TM AA Chromosomal Location Gene Symbol Gene Name Reference
Human 1 1210 7p12 EGFR epidermal growth factor receptor
Mouse 1 1210 11 A1-A4 Egfr epidermal growth factor receptor
Rat - 1209 14q22 Egfr epidermal growth factor receptor
Previous and Unofficial Names
EGF
HER1
ERBB
ERBB1
epidermal growth factor receptor (avian erythroblastic leukemia viral (v-erb-b) oncogene homolog)
erythroblastic leukemia viral (v-erb-b) oncogene homolog (avian)
ErbB-1
Errp
EGFR-related peptide
Epidermal growth factor receptor formerly avian erythroblastic leukemia viral (v-erbB) oncogene homolog (Erbb1)
Epidermal growth factor receptor, formerly avian erythroblastic leukemia viral (v-erbB) oncogene homolog (Erbb1)
avian erythroblastic leukemia viral (v-erbB) oncogene homolog
avian erythroblastic leukemia viral (v-erb-b) oncogene homolog
Wa5
Errb1
Egfr-related peptide
Erbb
epidermal growth factor receptor (erythroblastic leukemia viral (v-erb-b) oncogene homolog, avian)
ErbB1
Database Links
BRENDA
Ensembl Gene
Entrez Gene
ExplorEnz
GeneCards
GenitoUrinary Development Molecular Anatomy Project
HomoloGene
Human Protein Reference Database
InterPro
KEGG BRITE Hierarchy
KEGG Gene
OMIM
Orphanet Gene
PhosphoSitePlus
RefSeq Nucleotide
RefSeq Protein
TreeFam
UniGene
UniProtKB
Wikipedia
Selected 3D Structures
Image of receptor 3D structure from RCSB PDB
Description:  EGFR kinase domain complexed with a quinazoline inhibitor- GW572016
PDB Id:  1XKK
Ligand:  lapatinib
Resolution:  2.4Å
Species:  Human
References:  8
Image of receptor 3D structure from RCSB PDB
Description:  Crystal Structure of the Complex of Human Epidermal Growth Factor and Receptor Extracellular Domains.
PDB Id:  1IVO
Resolution:  3.3Å
Species:  Human
References:  4
Enzyme Reaction
EC Number: 2.7.10.1
Inhibitors
Key to terms and symbols View all chemical structures Click column headers to sort
Ligand Sp. Action Affinity Units Reference
gefitinib Hs Inhibition 8.3 pKi 6
pKi 8.3 (Ki 5.5x10-9 M) [6]
lapatinib Hs Inhibition 8.0 pIC50 5
pIC50 8.0 (IC50 1.02x10-8 M) [5]
Antibodies
Key to terms and symbols Click column headers to sort
Antibody Sp. Action Affinity Units Reference
cetuximab Hs Inhibition - -
panitumumab Hs Inhibition - -
DiscoveRx KINOMEscan® screen
A screen of 72 inhibitors against 456 human kinases. Quantitative data were derived using DiscoveRx KINOMEscan® platform.
http://www.discoverx.com/services/drug-discovery-development-services/kinase-profiling/kinomescan
Reference: 2,7

Key to terms and symbols Click column headers to sort
Target used in screen: EGFR
Ligand Sp. Type Action Affinity Units
canertinib Hs Inhibitor Inhibition 9.72 pKd
afatinib Hs Inhibitor Inhibition 9.6 pKd
erlotinib Hs Inhibitor Inhibition 9.17 pKd
gefitinib Hs Inhibitor Inhibition 9.0 pKd
neratinib Hs Inhibitor Inhibition 8.96 pKd
lapatinib Hs Inhibitor Inhibition 8.62 pKd
vandetanib Hs Inhibitor Inhibition 8.02 pKd
bosutinib Hs Inhibitor Inhibition 7.46 pKd
dasatinib Hs Inhibitor Inhibition 6.92 pKd
TAE 684 Hs Inhibitor Inhibition 6.74 pKd
Target used in screen: EGFR(E746-A750del)
Ligand Sp. Type Action Affinity Units
afatinib Hs Inhibitor Inhibition 9.96 pKd
canertinib Hs Inhibitor Inhibition 9.59 pKd
erlotinib Hs Inhibitor Inhibition 9.32 pKd
gefitinib Hs Inhibitor Inhibition 9.27 pKd
neratinib Hs Inhibitor Inhibition 8.64 pKd
vandetanib Hs Inhibitor Inhibition 8.32 pKd
lapatinib Hs Inhibitor Inhibition 8.07 pKd
bosutinib Hs Inhibitor Inhibition 7.74 pKd
TAE 684 Hs Inhibitor Inhibition 7.09 pKd
staurosporine Hs Inhibitor Inhibition 6.92 pKd
Target used in screen: EGFR(G719C)
Ligand Sp. Type Action Affinity Units
afatinib Hs Inhibitor Inhibition 10.0 pKd
canertinib Hs Inhibitor Inhibition 9.89 pKd
neratinib Hs Inhibitor Inhibition 9.43 pKd
erlotinib Hs Inhibitor Inhibition 9.07 pKd
lapatinib Hs Inhibitor Inhibition 9.04 pKd
gefitinib Hs Inhibitor Inhibition 8.7 pKd
vandetanib Hs Inhibitor Inhibition 8.02 pKd
bosutinib Hs Inhibitor Inhibition 7.01 pKd
barasertib-hQPA Hs Inhibitor Inhibition 6.92 pKd
foretinib Hs Inhibitor Inhibition 6.92 pKd
Target used in screen: EGFR(G719S)
Ligand Sp. Type Action Affinity Units
afatinib Hs Inhibitor Inhibition 9.72 pKd
canertinib Hs Inhibitor Inhibition 9.72 pKd
erlotinib Hs Inhibitor Inhibition 9.28 pKd
neratinib Hs Inhibitor Inhibition 9.04 pKd
gefitinib Hs Inhibitor Inhibition 8.96 pKd
lapatinib Hs Inhibitor Inhibition 8.68 pKd
vandetanib Hs Inhibitor Inhibition 8.23 pKd
bosutinib Hs Inhibitor Inhibition 7.59 pKd
dasatinib Hs Inhibitor Inhibition 7.1 pKd
cediranib Hs Inhibitor Inhibition 7.08 pKd
Target used in screen: EGFR(L747-E749del, A750P)
Ligand Sp. Type Action Affinity Units
afatinib Hs Inhibitor Inhibition 9.85 pKd
canertinib Hs Inhibitor Inhibition 9.77 pKd
erlotinib Hs Inhibitor Inhibition 9.28 pKd
gefitinib Hs Inhibitor Inhibition 9.24 pKd
neratinib Hs Inhibitor Inhibition 9.21 pKd
lapatinib Hs Inhibitor Inhibition 8.66 pKd
vandetanib Hs Inhibitor Inhibition 7.92 pKd
bosutinib Hs Inhibitor Inhibition 7.54 pKd
TAE 684 Hs Inhibitor Inhibition 7.14 pKd
staurosporine Hs Inhibitor Inhibition 7.02 pKd
Target used in screen: EGFR(L747-S752del, P753S)
Ligand Sp. Type Action Affinity Units
afatinib Hs Inhibitor Inhibition 9.92 pKd
canertinib Hs Inhibitor Inhibition 9.59 pKd
erlotinib Hs Inhibitor Inhibition 9.33 pKd
gefitinib Hs Inhibitor Inhibition 9.24 pKd
neratinib Hs Inhibitor Inhibition 9.03 pKd
lapatinib Hs Inhibitor Inhibition 8.41 pKd
vandetanib Hs Inhibitor Inhibition 8.1 pKd
bosutinib Hs Inhibitor Inhibition 7.42 pKd
TAE 684 Hs Inhibitor Inhibition 6.96 pKd
foretinib Hs Inhibitor Inhibition 6.68 pKd
Target used in screen: EGFR(L747-T751del,Sins)
Ligand Sp. Type Action Affinity Units
afatinib Hs Inhibitor Inhibition 9.92 pKd
canertinib Hs Inhibitor Inhibition 9.59 pKd
erlotinib Hs Inhibitor Inhibition 9.46 pKd
gefitinib Hs Inhibitor Inhibition 9.28 pKd
neratinib Hs Inhibitor Inhibition 9.0 pKd
lapatinib Hs Inhibitor Inhibition 8.46 pKd
vandetanib Hs Inhibitor Inhibition 8.05 pKd
bosutinib Hs Inhibitor Inhibition 7.52 pKd
TAE 684 Hs Inhibitor Inhibition 7.1 pKd
foretinib Hs Inhibitor Inhibition 6.8 pKd
Target used in screen: EGFR(L858R)
Ligand Sp. Type Action Affinity Units
afatinib Hs Inhibitor Inhibition 9.7 pKd
canertinib Hs Inhibitor Inhibition 9.62 pKd
neratinib Hs Inhibitor Inhibition 9.17 pKd
gefitinib Hs Inhibitor Inhibition 9.03 pKd
erlotinib Hs Inhibitor Inhibition 9.01 pKd
lapatinib Hs Inhibitor Inhibition 8.55 pKd
vandetanib Hs Inhibitor Inhibition 8.06 pKd
bosutinib Hs Inhibitor Inhibition 7.64 pKd
TAE 684 Hs Inhibitor Inhibition 7.34 pKd
dasatinib Hs Inhibitor Inhibition 6.92 pKd
Target used in screen: EGFR(L858R,T790M)
Ligand Sp. Type Action Affinity Units
canertinib Hs Inhibitor Inhibition 9.55 pKd
staurosporine Hs Inhibitor Inhibition 9.46 pKd
afatinib Hs Inhibitor Inhibition 8.96 pKd
TAE 684 Hs Inhibitor Inhibition 8.47 pKd
lestaurtinib Hs Inhibitor Inhibition 8.11 pKd
midostaurin Hs Inhibitor Inhibition 8.06 pKd
neratinib Hs Inhibitor Inhibition 7.57 pKd
R406 Hs Inhibitor Inhibition 7.21 pKd
gefitinib Hs Inhibitor Inhibition 6.85 pKd
GSK-1838705A Hs Inhibitor Inhibition 6.82 pKd
Target used in screen: EGFR(L861Q)
Ligand Sp. Type Action Affinity Units
canertinib Hs Inhibitor Inhibition 9.66 pKd
afatinib Hs Inhibitor Inhibition 9.64 pKd
neratinib Hs Inhibitor Inhibition 9.43 pKd
lapatinib Hs Inhibitor Inhibition 8.92 pKd
erlotinib Hs Inhibitor Inhibition 8.92 pKd
gefitinib Hs Inhibitor Inhibition 8.85 pKd
vandetanib Hs Inhibitor Inhibition 7.96 pKd
bosutinib Hs Inhibitor Inhibition 7.15 pKd
foretinib Hs Inhibitor Inhibition 7.07 pKd
TAE 684 Hs Inhibitor Inhibition 7.01 pKd
Target used in screen: EGFR(S752-I759del)
Ligand Sp. Type Action Affinity Units
afatinib Hs Inhibitor Inhibition 9.85 pKd
canertinib Hs Inhibitor Inhibition 9.72 pKd
neratinib Hs Inhibitor Inhibition 9.2 pKd
gefitinib Hs Inhibitor Inhibition 9.01 pKd
erlotinib Hs Inhibitor Inhibition 8.8 pKd
lapatinib Hs Inhibitor Inhibition 8.38 pKd
vandetanib Hs Inhibitor Inhibition 7.92 pKd
bosutinib Hs Inhibitor Inhibition 6.96 pKd
staurosporine Hs Inhibitor Inhibition 6.54 pKd
dasatinib Hs Inhibitor Inhibition 6.48 pKd
Target used in screen: EGFR(T790M)
Ligand Sp. Type Action Affinity Units
canertinib Hs Inhibitor Inhibition 10.0 pKd
afatinib Hs Inhibitor Inhibition 9.21 pKd
staurosporine Hs Inhibitor Inhibition 9.11 pKd
neratinib Hs Inhibitor Inhibition 8.82 pKd
TAE 684 Hs Inhibitor Inhibition 8.15 pKd
midostaurin Hs Inhibitor Inhibition 8.01 pKd
lestaurtinib Hs Inhibitor Inhibition 7.8 pKd
gefitinib Hs Inhibitor Inhibition 7.4 pKd
R406 Hs Inhibitor Inhibition 7.14 pKd
GSK-1838705A Hs Inhibitor Inhibition 7.13 pKd
Displaying the top 10 most potent ligands  View all ligands in screen »
EMD Millipore KinaseProfilerTM screen/Reaction Biology Kinase HotspotSM screen
A screen profiling 158 kinase inhibitors (Calbiochem Protein Kinase Inhibitor Library I and II, catalogue numbers 539744 and 539745) for their inhibitory activity at 1µM and 10µM against 234 human recombinant kinases using the EMD Millipore KinaseProfilerTM service.

A screen profiling the inhibitory activity of 178 commercially available kinase inhibitors at 0.5µM against a panel of 300 recombinant protein kinases using the Reaction Biology Corporation Kinase HotspotSM platform.

http://www.millipore.com/techpublications/tech1/pf3036
http://www.reactionbiology.com/webapps/main/pages/kinase.aspx


Reference: 1,3

Key to terms and symbols Click column headers to sort
Target used in screen: EGFR/EGFR
Ligand Sp. Type Action % Activity remaining at 0.5µM % Activity remaining at 1µM % Activity remaining at 10µM
AG1478 Hs Inhibitor Inhibition 0.7 -5.0 -3.0
EGFR/ErbB-2/ErbB-4 inhibitor Hs Inhibitor Inhibition 1.2 -4.0 -3.0
PD 158780 Hs Inhibitor Inhibition 2.0 -2.0 -3.0
compound 56 (PMID:8568816) Hs Inhibitor Inhibition 2.0 -5.0 -4.0
PD 174265 Hs Inhibitor Inhibition 2.2 -3.0 -3.0
JAK3 inhibitor II Hs Inhibitor Inhibition 2.2 -4.0 -3.0
gefitinib Hs Inhibitor Inhibition 3.0
BPIQ-I Hs Inhibitor Inhibition 3.6 -4.0 -3.0
bosutinib Hs Inhibitor Inhibition 3.8
erlotinib Hs Inhibitor Inhibition 4.2
Displaying the top 10 most potent ligands  View all ligands in screen »
Clinically-Relevant Mutations and Pathophysiology
Disease:  Lung cancer; Giant cell glioblastoma
OMIM:  211980
Orphanet:  251579
References: 
Mutations not determined
Disease:  Lung cancer; Gliosarcoma
OMIM:  211980
Orphanet:  251576
References: 
Mutations not determined

References

Show »

1. Anastassiadis T, Deacon SW, Devarajan K, Ma H, Peterson JR. (2011) Comprehensive assay of kinase catalytic activity reveals features of kinase inhibitor selectivity. Nat. Biotechnol.29 (11): 1039-45. [PMID:22037377]

2. Davis MI, Hunt JP, Herrgard S, Ciceri P, Wodicka LM, Pallares G, Hocker M, Treiber DK, Zarrinkar PP. (2011) Comprehensive analysis of kinase inhibitor selectivity. Nat. Biotechnol.29 (11): 1046-51. [PMID:22037378]

3. Gao Y, Davies SP, Augustin M, Woodward A, Patel UA, Kovelman R, Harvey KJ. (2013) A broad activity screen in support of a chemogenomic map for kinase signalling research and drug discovery. Biochem. J.451 (2): 313-28. [PMID:23398362]

4. Ogiso H, Ishitani R, Nureki O, Fukai S, Yamanaka M, Kim JH, Saito K, Sakamoto A, Inoue M, Shirouzu M et al.. (2002) Crystal structure of the complex of human epidermal growth factor and receptor extracellular domains. Cell110 (6): 775-87. [PMID:12297050]

5. Rusnak DW, Lackey K, Affleck K, Wood ER, Alligood KJ, Rhodes N, Keith BR, Murray DM, Knight WB, Mullin RJ et al.. (2001) The effects of the novel, reversible epidermal growth factor receptor/ErbB-2 tyrosine kinase inhibitor, GW2016, on the growth of human normal and tumor-derived cell lines in vitro and in vivo. Mol. Cancer Ther.1 (2): 85-94. [PMID:12467226]

6. Wissner A, Fraser HL, Ingalls CL, Dushin RG, Floyd MB, Cheung K, Nittoli T, Ravi MR, Tan X, Loganzo F. (2007) Dual irreversible kinase inhibitors: quinazoline-based inhibitors incorporating two independent reactive centers with each targeting different cysteine residues in the kinase domains of EGFR and VEGFR-2. Bioorg. Med. Chem.15 (11): 3635-48. [PMID:17416531]

7. Wodicka LM, Ciceri P, Davis MI, Hunt JP, Floyd M, Salerno S, Hua XH, Ford JM, Armstrong RC, Zarrinkar PP et al.. (2010) Activation state-dependent binding of small molecule kinase inhibitors: structural insights from biochemistry. Chem. Biol.17 (11): 1241-9. [PMID:21095574]

8. Wood ER, Truesdale AT, McDonald OB, Yuan D, Hassell A, Dickerson SH, Ellis B, Pennisi C, Horne E, Lackey K et al.. (2004) 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.64 (18): 6652-9. [PMID:15374980]

How to cite this page

Receptor tyrosine kinases: epidermal growth factor receptor. Last modified on 11/03/2014. Accessed on 19/04/2014. IUPHAR/BPS Guide to PHARMACOLOGY, http://www.guidetopharmacology.org/GRAC/ObjectDisplayForward?objectId=1797.