Id: | acc0129 |
Group: | 1sens_supp |
Protein: | EGFR |
Gene Symbol: | EGFR |
Protein Id: | P00533 |
Protein Name: | EGFR_HUMAN |
PTM: | phosphorylation |
Site: | Tyr1173 |
Site Sequence: | QISLDNPDYQQDFFPKEAKPN |
Disease Category: | Cancer |
Disease: | Breast Cancer |
Disease Subtype: | |
Disease Cellline: | MDA-MB-231 |
Disease Info: | |
Drug: | erlotinib |
Drug Info: | "Erlotinib is a medication used in the treatment of certain types of lung cancer, particularly non-small cell lung cancer (NSCLC), and pancreatic cancer, often as a maintenance therapy or after chemotherapy failure." |
Effect: | increase |
Effect Info: | "Injecting INCB3619 into tumor-bearing mice can inhibit the signal transduction of the ErbB pathway (such as the phosphorylation of Akt), as well as the proliferation and survival of tumor cells." |
Note: | |
Score: | 5.0 |
Pubmed(PMID): | 17363546 |
Sentence Index: | 17363546_9 |
Sentence: | Therapeutic benefit was obtained without notation of compounding toxicity. Similar results have been obtained using erlotinib in place of gefitinib (data not shown). These data are consistent with that recently published exemplifying the ability of INCB3619 to potentiate the effects of gefitinib in vitro. |
Sequence & Structure:
MRPSGTAGAALLALLAALCPASRALEEKKVCQGTSNKLTQLGTFEDHFLSLQRMFNNCEVVLGNLEITYVQRNYDLSFLKTIQEVAGYVLIALNTVERIPLENLQIIRGNMYYENSYALAVLSNYDANKTGLKELPMRNLQEILHGAVRFSNNPALCNVESIQWRDIVSSDFLSNMSMDFQNHLGSCQKCDPSCPNGSCWGAGEENCQKLTKIICAQQCSGRCRGKSPSDCCHNQCAAGCTGPRESDCLVCRKFRDEATCKDTCPPLMLYNPTTYQMDVNPEGKYSFGATCVKKCPRNYVVTDHGSCVRACGADSYEMEEDGVRKCKKCEGPCRKVCNGIGIGEFKDSLSINATNIKHFKNCTSISGDLHILPVAFRGDSFTHTPPLDPQELDILKTVKEITGFLLIQAWPENRTDLHAFENLEIIRGRTKQHGQFSLAVVSLNITSLGLRSLKEISDGDVIISGNKNLCYANTINWKKLFGTSGQKTKIISNRGENSCKATGQVCHALCSPEGCWGPEPRDCVSCRNVSRGRECVDKCNLLEGEPREFVENSECIQCHPECLPQAMNITCTGRGPDNCIQCAHYIDGPHCVKTCPAGVMGENNTLVWKYADAGHVCHLCHPNCTYGCTGPGLEGCPTNGPKIPSIATGMVGALLLLLVVALGIGLFMRRRHIVRKRTLRRLLQERELVEPLTPSGEAPNQALLRILKETEFKKIKVLGSGAFGTVYKGLWIPEGEKVKIPVAIKELREATSPKANKEILDEAYVMASVDNPHVCRLLGICLTSTVQLITQLMPFGCLLDYVREHKDNIGSQYLLNWCVQIAKGMNYLEDRRLVHRDLAARNVLVKTPQHVKITDFGLAKLLGAEEKEYHAEGGKVPIKWMALESILHRIYTHQSDVWSYGVTVWELMTFGSKPYDGIPASEISSILEKGERLPQPPICTIDVYMIMVKCWMIDADSRPKFRELIIEFSKMARDPQRYLVIQGDERMHLPSPTDSNFYRALMDEEDMDDVVDADEYLIPQQGFFSSPSTSRTPLLSSLSATSNNSTVACIDRNGLQSCPIKEDSFLQRYSSDPTGALTEDSIDDTFLPVPEYINQSVPKRPAGSVQNPVYHNQPLNPAPSRDPHYQDPHSTAVGNPEYLNTVQPTCVNSTFDSPAHWAQKGSHQISLDNPDYQQDFFPKEAKPNGIFKGSTAENAEYLRVAPQSSEFIGA
Select PDB:
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 TargetsPTM Intensity:
source: CPTACNo 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: PTMDResidue | Position | State | Disease | Class | PMID |
---|---|---|---|---|---|
Y | 1173 | U | Non-small cell lung cancer/carcinoma | Phosphorylation | 19002495 |
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: DecryptMNo data.
Function score:
source: funscoRNo data.