Id: acc5134
Group: 1sens
Protein: EGFR
Gene Symbol: Egfr
Protein Id: P00533
Protein Name: EGFR_HUMAN
PTM: phosphorylation
Site: Tyr1068
Site Sequence: PIKEDSFLQRYSSDPTGALTE
Disease Category: Nervous system diseases
Disease: Spinal Cord Injury
Disease Subtype: primary traumatic spinal cord injury
Disease Cellline:
Disease Info:
Drug: AG1478
Drug Info: "AG1478 is a potent and selective inhibitor of the epidermal growth factor receptor (EGFR) tyrosine kinase, which has been widely used in cancer research to study the role of EGFR signaling pathways."
Effect: modulate
Effect Info: "Inhibition of EGFR phosphorylation using C225 or AG1478, and significant EGFR blockade reduced MAPK activation, decreased nerve inflammation-related damage, and promoted axonal growth and functional recovery."
Note:
Score: 4.0
Pubmed(PMID): 22824323
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 data.

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: