Id: | acc1673 |
Group: | 2sens |
Protein: | EGFR |
Gene Symbol: | EGFR |
Protein Id: | P00533 |
Protein Name: | EGFR_HUMAN |
PTM: | phosphorylation |
Site: | unclear |
Site Sequence: | |
Disease Category: | Cancer |
Disease: | Thyroid Cancer |
Disease Subtype: | |
Disease Cellline: | |
Disease Info: | |
Drug: | Apigenin |
Drug Info: | "Apigenin is a naturally occurring flavonoid compound with demonstrated potential as an antifungal agent in the preparation of drugs against human fungal infections, and it is also being researched in drug delivery systems such as solid lipid nanoparticles (APG-SLNP) to enhance stability and bioavailability. " |
Relation: |
Apigenin
➜
EGFR-unclear
DOWN
➜
Thyroid Cancer
Alleviate
|
Effect: | modulate |
Effect Info: | Apigenin inhibits the growth of thyroid cancer cells by suppressing the tyrosine phosphorylation of epidermal growth factor receptor (EGF - R) and the phosphorylation of ERK mitogen - activated protein (MAP) kinase. |
Note: | |
Score: | 4.0 |
Pubmed(PMID): | 11299771 |
Sentence Index: | 11299771_1-2 |
Sentence: | "We have previously reported that apigenin inhibits the growth of thyroid cancer cells by attenuating epidermal growth factor receptor (EGF-R) tyrosine phosphorylation and phosphorylation of ERK mitogen-activated protein (MAP) kinase. In this study, we assessed the growth inhibitory effect of apigenin on MCF-7 breast carcinoma cells that express two key cell cycle regulators, wild-type p53 and the retinoblastoma tumor suppressor protein (Rb), and MDA-MB-468 breast carcinoma cells that are mutant for p53 and Rb negative." |
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 |
---|---|---|---|---|---|
- | - | A | B-cell chronic lymphocytic leukemia | Phosphorylation | 23866081 |
- | - | A | Lung adenocarcinoma | Phosphorylation | 23866081 |
- | - | A | Renal tubulointerstitial fibrosis | Ubiquitination | 32017279 |
- | - | D | Gastric adenocarcinoma | Glycosylation | 30323967 |
- | - | D | Bladder cancer | Ubiquitination | 33253711 |
- | - | D | Osteosarcoma | Ubiquitination | 32775001 |
- | - | D | Breast cancer | Ubiquitination | 31801577 |
- | - | D | Lung adenocarcinoma | Ubiquitination | 37240137 |
- | - | D | Cardiac hypertrophy | Ubiquitination | 32494592 |
- | - | D | Thyroid cancer/carcinoma | Phosphorylation | 16822827 |
- | - | P | B-cell chronic lymphocytic leukemia | Phosphorylation | 23866081 |
- | - | P | Lung adenocarcinoma | Phosphorylation | 23866081 |
- | - | P | Epidermoid carcinoma | Phosphorylation | 23499740 |
- | - | P | Thyroid cancer/carcinoma | Phosphorylation | 11299771 |
- | - | U | Ovarian cancer/carcinoma | Phosphorylation | 22952709 |
- | - | U | Head and neck squamous cell carcinoma | Phosphorylation | 23799848 |
- | - | U | Colon cancer/carcinoma | Phosphorylation | 24665413 |
- | - | U | Breast cancer | Ubiquitination | 36841821 |
- | - | U | Hepatocellular carcinoma | Ubiquitination | 32382041 |
- | - | U | Gastric cancer | Ubiquitination | 34034092 |
- | - | U | Glioma | Phosphorylation | 24403856 |
- | - | U | Hepatocellular carcinoma | Ubiquitination | 33116595 |
- | - | U | Glioblastoma | Ubiquitination | 36335869 |
- | - | U | Non-small cell lung cancer | Phosphorylation | 36896765 |
- | - | U | Follicular thyroid carcinoma | Glycosylation | 32442537 |
- | - | U | Head and neck squamous cell carcinoma | Glycosylation | 29930379 |
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.