Id: acc1100
Group: 2sens
Protein: EGFR
Gene Symbol: EGFR
Protein Id: P00533
Protein Name: EGFR_HUMAN
PTM: phosphorylation
Site: Tyr1068
Site Sequence: PIKEDSFLQRYSSDPTGALTE
Disease Category: Cancer
Disease: Lung Cancer
Disease Subtype: NSCLC
Disease Cellline: PC-9/GR
Disease Info:
Drug: gefitinib + Lovastatin
Drug Info: Gefitinib: - Lovastatin: Lovastatin is a cell-permeable HMG-CoA reductase inhibitor used to lower cholesterol.
Effect: modulate
Effect Info: "Lovastatin inhibits cholesterol synthesis, rendering gefitinib-resistant cell lines sensitive to gefitinib. The combined use significantly inhibits the phosphorylation of EGFR, Akt - 1, MEK1/2, and ERK1/2."
Note: drug comb
Score: 4.0
Pubmed(PMID): 29215723
Sentence Index:
Sentence:

Sequence & Structure:

MRPSGTAGAALLALLAALCPASRALEEKKVCQGTSNKLTQLGTFEDHFLSLQRMFNNCEVVLGNLEITYVQRNYDLSFLKTIQEVAGYVLIALNTVERIPLENLQIIRGNMYYENSYALAVLSNYDANKTGLKELPMRNLQEILHGAVRFSNNPALCNVESIQWRDIVSSDFLSNMSMDFQNHLGSCQKCDPSCPNGSCWGAGEENCQKLTKIICAQQCSGRCRGKSPSDCCHNQCAAGCTGPRESDCLVCRKFRDEATCKDTCPPLMLYNPTTYQMDVNPEGKYSFGATCVKKCPRNYVVTDHGSCVRACGADSYEMEEDGVRKCKKCEGPCRKVCNGIGIGEFKDSLSINATNIKHFKNCTSISGDLHILPVAFRGDSFTHTPPLDPQELDILKTVKEITGFLLIQAWPENRTDLHAFENLEIIRGRTKQHGQFSLAVVSLNITSLGLRSLKEISDGDVIISGNKNLCYANTINWKKLFGTSGQKTKIISNRGENSCKATGQVCHALCSPEGCWGPEPRDCVSCRNVSRGRECVDKCNLLEGEPREFVENSECIQCHPECLPQAMNITCTGRGPDNCIQCAHYIDGPHCVKTCPAGVMGENNTLVWKYADAGHVCHLCHPNCTYGCTGPGLEGCPTNGPKIPSIATGMVGALLLLLVVALGIGLFMRRRHIVRKRTLRRLLQERELVEPLTPSGEAPNQALLRILKETEFKKIKVLGSGAFGTVYKGLWIPEGEKVKIPVAIKELREATSPKANKEILDEAYVMASVDNPHVCRLLGICLTSTVQLITQLMPFGCLLDYVREHKDNIGSQYLLNWCVQIAKGMNYLEDRRLVHRDLAARNVLVKTPQHVKITDFGLAKLLGAEEKEYHAEGGKVPIKWMALESILHRIYTHQSDVWSYGVTVWELMTFGSKPYDGIPASEISSILEKGERLPQPPICTIDVYMIMVKCWMIDADSRPKFRELIIEFSKMARDPQRYLVIQGDERMHLPSPTDSNFYRALMDEEDMDDVVDADEYLIPQQGFFSSPSTSRTPLLSSLSATSNNSTVACIDRNGLQSCPIKEDSFLQRYSSDPTGALTEDSIDDTFLPVPEYINQSVPKRPAGSVQNPVYHNQPLNPAPSRDPHYQDPHSTAVGNPEYLNTVQPTCVNSTFDSPAHWAQKGSHQISLDNPDYQQDFFPKEAKPNGIFKGSTAENAEYLRVAPQSSEFIGA

Select PDB:

Known Drugs:

source: Multi-Sources

(see table)

Target Drug name MOA Phase Status Disease Source
EGFR LAPATINIB DITOSYLATE Epidermal growth factor receptor erbB1 inhibitor 4 - breast carcinoma FDA
EGFR NERATINIB MALEATE Epidermal growth factor receptor erbB1 inhibitor 4 - breast carcinoma FDA
EGFR CETUXIMAB Epidermal growth factor receptor erbB1 inhibitor 4 - colorectal adenocarcinoma DailyMed
EGFR PANITUMUMAB Epidermal growth factor receptor erbB1 inhibitor 4 - colorectal adenocarcinoma DailyMed
EGFR NECITUMUMAB Epidermal growth factor receptor erbB1 inhibitor 4 - neoplasm ATC
EGFR AMIVANTAMAB Epidermal growth factor receptor inhibitor 4 - neoplasm ATC
EGFR CETUXIMAB Epidermal growth factor receptor erbB1 inhibitor 4 - neoplasm ATC
EGFR CETUXIMAB Epidermal growth factor receptor erbB1 inhibitor 4 Recruiting neoplasm ClinicalTrials
EGFR VANDETANIB Epidermal growth factor receptor inhibitor 4 - neoplasm ATC
EGFR PANITUMUMAB Epidermal growth factor receptor erbB1 inhibitor 4 - neoplasm ATC
EGFR GEFITINIB Epidermal growth factor receptor erbB1 inhibitor 4 - neoplasm ATC
EGFR DACOMITINIB Epidermal growth factor receptor erbB1 inhibitor 4 - neoplasm ATC
EGFR MOBOCERTINIB Epidermal growth factor receptor erbB1 inhibitor 4 - neoplasm ATC
EGFR OSIMERTINIB Epidermal growth factor receptor erbB1 inhibitor 4 - neoplasm ATC
EGFR BRIGATINIB Epidermal growth factor receptor erbB1 inhibitor 4 - neoplasm ATC
EGFR CETUXIMAB Epidermal growth factor receptor erbB1 inhibitor 4 - squamous cell carcinoma DailyMed
EGFR VANDETANIB Epidermal growth factor receptor inhibitor 4 - thyroid carcinoma DailyMed
EGFR NECITUMUMAB Epidermal growth factor receptor erbB1 inhibitor 4 - non-small cell lung carcinoma EMA
DailyMed
EGFR AFATINIB DIMALEATE Epidermal growth factor receptor erbB1 inhibitor 4 - non-small cell lung carcinoma DailyMed
EGFR AFATINIB DIMALEATE Epidermal growth factor receptor erbB1 inhibitor 4 Not yet recruiting non-small cell lung carcinoma ClinicalTrials
EGFR DACOMITINIB Epidermal growth factor receptor erbB1 inhibitor 4 - non-small cell lung carcinoma FDA
EMA
EGFR OSIMERTINIB MESYLATE Epidermal growth factor receptor erbB1 inhibitor 4 - non-small cell lung carcinoma EMA
DailyMed
EGFR ERLOTINIB HYDROCHLORIDE Epidermal growth factor receptor erbB1 inhibitor 4 - non-small cell lung carcinoma DailyMed
EGFR BRIGATINIB Epidermal growth factor receptor erbB1 inhibitor 4 - non-small cell lung carcinoma EMA
FDA
EGFR AMIVANTAMAB Epidermal growth factor receptor inhibitor 4 - non-small cell lung carcinoma EMA
FDA

Note: Only show clinically investigational or approved drugs with protein targets.

Protein Tractability:

source: Open Targets
Small molecule
Antibody
PROTAC
Other modalities
Approved Drug
Advanced Clinical
Phase 1 Clinical
Structure with Ligand
High-Quality Ligand
High-Quality Pocket
Med-Quality Pocket
Druggable Family
Approved Drug
Advanced Clinical
Phase 1 Clinical
UniProt loc high conf
GO CC high conf
UniProt loc med conf
UniProt SigP or TMHMM
GO CC med conf
Human Protein Atlas loc
Approved Drug
Advanced Clinical
Phase 1 Clinical
Literature
UniProt Ubiquitination
Database Ubiquitination
Half-life Data
Small Molecule Binder
Approved Drug
Advanced Clinical
Phase 1 Clinical

PTM Intensity:

source: CPTAC

No intensity data of this site,
show all other sites!

EGFR-Ser1012
Cancer Intensity
BRCA
COAD
HGSC
ccRCC -0.224
GBM
HNSC
LUAD 1.093
LUSC -0.869
non_ccRCC
PDAC
UCEC
EGFR-Ser1019
Cancer Intensity
BRCA -0.162
COAD 0.525
HGSC 1.91
ccRCC -0.216
GBM
HNSC
LUAD -1.07
LUSC -1.597
non_ccRCC -0.132
PDAC 0.291
UCEC 0.453
EGFR-Ser1026
Cancer Intensity
BRCA
COAD 0.707
HGSC
ccRCC
GBM
HNSC
LUAD -0.707
LUSC
non_ccRCC
PDAC
UCEC
EGFR-Ser1121
Cancer Intensity
BRCA
COAD 0.33
HGSC 0.793
ccRCC -1.123
GBM
HNSC
LUAD
LUSC
non_ccRCC
PDAC
UCEC
EGFR-Ser650
Cancer Intensity
BRCA
COAD -0.529
HGSC 1.453
ccRCC -0.792
GBM
HNSC
LUAD -1.019
LUSC -0.082
non_ccRCC
PDAC
UCEC 0.969
EGFR-Ser675
Cancer Intensity
BRCA -2.294
COAD
HGSC 0.643
ccRCC 0.535
GBM
HNSC
LUAD -0.009
LUSC -0.232
non_ccRCC 0.66
PDAC 0.738
UCEC -0.041
EGFR-Ser946
Cancer Intensity
BRCA 0.751
COAD 0.597
HGSC 1.404
ccRCC -0.059
GBM
HNSC
LUAD 0.114
LUSC -0.811
non_ccRCC -2.003
PDAC 0.462
UCEC -0.456
EGFR-Ser991
Cancer Intensity
BRCA
COAD
HGSC
ccRCC 0.707
GBM -0.707
HNSC
LUAD
LUSC
non_ccRCC
PDAC
UCEC
EGFR-Ser992
Cancer Intensity
BRCA
COAD
HGSC
ccRCC -0.707
GBM
HNSC 0.707
LUAD
LUSC
non_ccRCC
PDAC
UCEC
EGFR-Ser994
Cancer Intensity
BRCA
COAD 0.623
HGSC -0.784
ccRCC -0.58
GBM
HNSC
LUAD -0.129
LUSC
non_ccRCC -1.376
PDAC 0.785
UCEC 1.461
EGFR-Ser997
Cancer Intensity
BRCA 1.611
COAD 0.359
HGSC -2.065
ccRCC -0.131
GBM
HNSC
LUAD 0.009
LUSC -0.098
non_ccRCC 0.862
PDAC -0.488
UCEC -0.059
EGFR-Thr648
Cancer Intensity
BRCA 1.108
COAD 0.434
HGSC 1.068
ccRCC 0.044
GBM
HNSC
LUAD 0.416
LUSC -1.175
non_ccRCC -1.717
PDAC -0.77
UCEC 0.592
EGFR-Thr948
Cancer Intensity
BRCA
COAD 0.914
HGSC 0.483
ccRCC -0.006
GBM
HNSC
LUAD -1.39
LUSC
non_ccRCC
PDAC
UCEC
EGFR-Thr996
Cancer Intensity
BRCA 1.232
COAD -0.247
HGSC
ccRCC -1.249
GBM
HNSC
LUAD -0.683
LUSC -0.608
non_ccRCC 1.709
PDAC -0.291
UCEC 0.136
EGFR-Tyr1047
Cancer Intensity
BRCA
COAD 0.614
HGSC
ccRCC 0.139
GBM
HNSC
LUAD -0.763
LUSC -1.224
non_ccRCC
PDAC
UCEC 1.234
EGFR-Tyr1127
Cancer Intensity
BRCA 0.853
COAD 0.567
HGSC 1.203
ccRCC -0.756
GBM
HNSC
LUAD -0.922
LUSC -0.649
non_ccRCC -1.614
PDAC 0.354
UCEC 0.964
EGFR-Tyr1152
Cancer Intensity
BRCA 0.302
COAD 0.15
HGSC 0.898
ccRCC -0.139
GBM
HNSC
LUAD -0.637
LUSC -1.754
non_ccRCC -0.871
PDAC 0.427
UCEC 1.624

PTM-Disease Association:

source: PTMD
Residue Position State Disease Class PMID
Y 1068 D Glioblastoma multiforme Phosphorylation 35915159
Y 1068 P Gastric cancer Phosphorylation 23613900
Y 1068 P Tonsillar cancer Phosphorylation 23564800
Y 1068 U Non-small cell lung cancer/carcinoma Phosphorylation 22901364 ;  18687633
Y 1068 U Prostate cancer/carcinoma/adenocarcinoma Phosphorylation 22307624
Y 1068 U Squamous cell carcinoma Phosphorylation 37109043
Y 1068 U Pancreatic cancer Phosphorylation 31851779

State Note: Based on the distinct PTM states in diseases, PTMD classified all disease-associated PTMs into six classes, including whether the up-regulation (U) or down-regulation (D) of PTM levels, the absence (A) or presence (P) of PTMs, and the creation (C) or disruption (N) of PTM sites are associated with diseases.

PTM-Drug Perturbation Response:

source: DecryptM

No data.

Function score:

source: funscoR

No data.

Cross Links: